2024

Quon, T., Lin, L.-C., Ganguly, A. , Hudson, B. D. , Tobin, A. B. and Milligan, G. (2024) Biased constitutive signalling of the G protein-coupled receptor GPR35 suppresses gut barrier permeability. Journal of Biological Chemistry, (Accepted for Publication)

Brettell, S. B. et al. (2024) Targeting PfCLK3 with covalent inhibitors: a novel strategy for malaria treatment. Journal of Medicinal Chemistry, (doi: 10.1021/acs.jmedchem.4c01300) (PMID:39441986) (Early Online Publication)

Marsango, S. and Milligan, G. (2024) Regulation of the pro-inflammatory G protein-coupled receptor GPR84. British Journal of Pharmacology, 181(10), pp. 1500-1508. (doi: 10.1111/bph.16098) (PMID:37085331)

Milligan, G. (2024) Editorial for GPR84 Pharmacology. British Journal of Pharmacology, 181(10), pp. 1497-1499. (doi: 10.1111/bph.16340)

Tikhonova, I., Zhang, X., Guseinov, A.-A., Jenkins, L. , Li, K., Milligan, G. and Zhang, C. (2024) Structural basis for the ligand recognition and signaling of free fatty acid receptors. Science Advances, 10(2), eadj2384. (doi: 10.1126/sciadv.adj2384) (PMID:38198545)

2023

Barki, N. et al. (2023) Phosphorylation bar-coding of free fatty acid receptor 2 is generated in a tissue-specific manner. eLife, 12, RP91861. (doi: 10.7554/eLife.91861) (PMID:38085667) (PMCID:PMC10715726)

Kalita, M. et al. (2023) PET imaging of innate immune activation using 11C radiotracers targeting GPR84. JACS Au, 3(12), pp. 3297-3310. (doi: 10.1021/jacsau.3c00435) (PMID:38155640) (PMCID:PMC10751761)

Ganguly, A. et al. (2023) G protein-receptor kinases 5/6 are the key regulators of G protein-coupled receptor 35-arrestin interactions. Journal of Biological Chemistry, 299(10), 105218. (doi: 10.1016/j.jbc.2023.105218) (PMID:37660910) (PMCID:PMC10520886)

Zhang, X. et al. (2023) Pro-phagocytic function and structural basis of GPR84 signaling. Nature Communications, 14, 5706. (doi: 10.1038/s41467-023-41201-0) (PMID:37709767) (PMCID:PMC10502086)

Valentini, A., Schultz-Knudsen, K., Højgaard Hansen, A., Tsakoumagkou, A., Jenkins, L. , Christensen, H. B., Manandhar, A., Milligan, G. , Ulven, T. and Rexen Ulven, E. (2023) Discovery of potent tetrazole free fatty acid receptor 2 antagonists. Journal of Medicinal Chemistry, 66(9), pp. 6105-6121. (doi: 10.1021/acs.jmedchem.2c01935) (PMID:37129317)

Milligan, G. (2023) GPR35: from enigma to therapeutic target. Trends in Pharmacological Sciences, 44(5), pp. 263-273. (doi: 10.1016/j.tips.2023.03.001) (PMID:37002007)

Meda Venkata, S. P., Li, H., Xu, L., Koh, J. Y., Nguyen, H., Minjares, M., Li, C., Kowluru, A., Milligan, G. and Wang, J.-M. (2023) Inhibition of GPR39 restores defects in endothelial cell–mediated neovascularization under the duress of chronic hyperglycemia: evidence for regulatory roles of the sonic hedgehog signaling axis. Proceedings of the National Academy of Sciences of the United States of America, 120(1), e2208541120. (doi: 10.1073/pnas.2208541120) (PMID:36574661) (PMCID:PMC9910611)

2022

Alharbi, A. G., Tobin, A. B. and Milligan, G. (2022) How arrestins and GRKs regulate the function of long chain fatty acid receptors. International Journal of Molecular Sciences, 23(20), 12237. (doi: 10.3390/ijms232012237) (PMID:36293091) (PMCID:PMC9602559)

Mahindra, A. et al. (2022) Investigating the structure–activity relationship of 1,2,4-triazine G-protein-coupled receptor 84 (GPR84) antagonists. Journal of Medicinal Chemistry, 65(16), pp. 11270-11290. (doi: 10.1021/acs.jmedchem.2c00804) (PMID:35948061) (PMCID:PMC9421653)

Marsango, S., Barki, N., Jenkins, L. , Tobin, A. B. and Milligan, G. (2022) Therapeutic validation of an orphan G protein-coupled receptor: the case of GPR84. British Journal of Pharmacology, 179(14), pp. 3529-3541. (doi: 10.1111/bph.15248) (PMID:32869860) (PMCID:PMC9361006)

Marsango, S. et al. (2022) The M1 muscarinic receptor is present in situ as a ligand-regulated mixture of monomers and oligomeric complexes. Proceedings of the National Academy of Sciences of the United States of America, 119(24), e220110311. (doi: 10.1073/pnas.2201103119) (PMID:35671422) (PMCID:PMC9214538)

Caspar, B., Cocchiara, P., Melet, A., Van Emelen, K., Van der Aa, A., Milligan, G. and Herbeuval, J.-P. (2022) CXCR4 as a novel target in immunology: moving away from typical antagonists. Future Drug Discovery, 4(2), FDD77. (doi: 10.4155/fdd-2022-0007) (PMID:35875591) (PMCID:PMC9298491)

Marsango, S. et al. (2022) Selective phosphorylation of threonine residues defines GPR84-arrestin interactions of biased ligands. Journal of Biological Chemistry, 298(5), 101932. (doi: 10.1016/j.jbc.2022.101932) (PMID:35427647) (PMCID:PMC9118924)

Barki, N. et al. (2022) Chemogenetics defines the roles of short chain fatty acid receptors within the gut-brain axis. eLife, 11, e73777. (doi: 10.7554/eLife.73777) (PMID:35229717) (PMCID:PMC8887895)

Divorty, N., Jenkins, L. , Ganguly, A. , Butcher, A. J., Hudson, B. D. , Schulz, S., Tobin, A. B. , Nicklin, S. A. and Milligan, G. (2022) Agonist-induced phosphorylation of orthologues of the orphan receptor GPR35 functions as an activation sensor. Journal of Biological Chemistry, 298(3), 101655. (doi: 10.1016/j.jbc.2022.101655) (PMID:35101446) (PMCID:PMC8892012)

2021

Scarpa, M. et al. (2021) Biased M1 muscarinic receptor mutant mice show accelerated progression of prion neurodegenerative disease. Proceedings of the National Academy of Sciences of the United States of America, 118(50), e2107389118. (doi: 10.1073/pnas.2107389118) (PMID:34893539) (PMCID:PMC8685681)

Lin, L.-C., Quon, T., Engberg, S., Mackenzie, A. E., Tobin, A. B. and Milligan, G. (2021) G protein-coupled receptor GPR35 suppresses lipid accumulation in hepatocytes. ACS Pharmacology and Translational Science, 4(6), pp. 1835-1848. (doi: 10.1021/acsptsci.1c00224) (PMID:34927014)

Milligan, G. et al. (2021) Discovery and characterization of novel antagonists of the proinflammatory orphan receptor GPR84. ACS Pharmacology and Translational Science, 4(5), pp. 1598-1613. (doi: 10.1021/acsptsci.1c00151) (PMID:34661077) (PMCID:PMC8506611)

Boleij, A. et al. (2021) G-protein coupled receptor 35 (GPR35) regulates the colonic epithelial cell response to enterotoxigenic Bacteroides fragilis. Communications Biology, 4, 585. (doi: 10.1038/s42003-021-02014-3) (PMID:33990686) (PMCID:PMC8121840)

Milligan, G. , Barki, N. and Tobin, A. (2021) Chemogenetic approaches to explore the functions of Free Fatty Acid Receptor 2. Trends in Pharmacological Sciences, 42(3), pp. 191-202. (doi: 10.1016/j.tips.2020.12.003) (PMID:33495026)

Bolognini, D., Dedeo, D. and Milligan, G. (2021) Metabolic and inflammatory functions of short-chain fatty acid receptors. Current Opinion in Endocrine and Metabolic Research, 16, pp. 1-9. (doi: 10.1016/j.coemr.2020.06.005) (PMID:32835130) (PMCID:PMC7332907)

Ward, R. J., Pediani, J. D. , Marsango, S., Jolly, R., Stoneman, M. R., Biener, G., Handel, T. M., Raicu, V. and Milligan, G. (2021) Chemokine receptor CXCR4 oligomerization is disrupted selectively by the antagonist ligand IT1t. Journal of Biological Chemistry, 296, 100139. (doi: 10.1074/jbc.RA120.016612) (PMID:33268380)

2020

Marti-Solano, M. et al. (2020) Combinatorial expression of GPCR isoforms affects signalling and drug responses. Nature, 587, pp. 650-656. (doi: 10.1038/s41586-020-2888-2) (PMID:33149304)

Labéguère, F. et al. (2020) Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a unique GPR84 negative allosteric modulator undergoing evaluation in a phase II clinical trial. Journal of Medicinal Chemistry, 63(22), pp. 13526-13545. (doi: 10.1021/acs.jmedchem.0c00272) (PMID:32902984)

Prihandoko, R. et al. (2020) Pathophysiological regulation of lung function by the free fatty acid receptor FFA4. Science Translational Medicine, 12(557), eaaw9009. (doi: 10.1126/scitranslmed.aaw9009) (PMID:32817367)

Quon, T., Lin, L.-C., Ganguly, A. , Tobin, A. B. and Milligan, G. (2020) Therapeutic opportunities and challenges in targeting the orphan G protein-coupled receptor GPR35. ACS Pharmacology and Translational Science, 3(5), pp. 801-812. (doi: 10.1021/acsptsci.0c00079) (PMID:33073184)

Rexen Ulven, E. et al. (2020) Structure-activity relationship studies of tetrahydroquinolone free fatty acid receptor 3 modulators. Journal of Medicinal Chemistry, 63(7), pp. 3577-3595. (doi: 10.1021/acs.jmedchem.9b02036) (PMID:32141297) (PMCID:PMC7307922)

Sencio, V. et al. (2020) Gut dysbiosis during influenza contributes to pulmonary pneumococcal superinfection through altered short-chain fatty acid production. Cell Reports, 30(9), 2934-2947.e6. (doi: 10.1016/j.celrep.2020.02.013) (PMID:32130898)

2019

Heuninck, J. et al. (2019) Context-dependent signaling of CXC chemokine receptor 4 and atypical chemokine receptor 3. Molecular Pharmacology, 96(6), pp. 778-793. (doi: 10.1124/mol.118.115477) (PMID:31092552)

Stoneman, M. R., Biener, G., Ward, R. J., Pediani, J. D. , Badu, D., Eis, A., Popa, I., Milligan, G. and Raicu, V. (2019) A general method to quantify ligand-driven oligomerization from fluorescence-based images. Nature Methods, 16(6), pp. 493-496. (doi: 10.1038/s41592-019-0408-9) (PMID:31110281)

Bolognini, D. et al. (2019) Chemogenetics defines receptor-mediated functions of short chain free fatty acids. Nature Chemical Biology, 15(5), pp. 489-498. (doi: 10.1038/s41589-019-0270-1) (PMID:30992568)

Mackenzie, A. E., Quon, T., Lin, L.-C., Hauser, A. S., Jenkins, L. , Inoue, A., Tobin, A. B. , Gloriam, D. E., Hudson, B. D. and Milligan, G. (2019) Receptor selectivity between the G proteins Gα12 and Gα13 is defined by a single leucine-to-isoleucine variation. FASEB Journal, 33(4), pp. 5005-5017. (doi: 10.1096/fj.201801956R) (PMID:30601679) (PMCID:PMC6436656)

Milligan, G. , Ward, R. J. and Marsango, S. (2019) GPCR homo-oligomerization. Current Opinion in Cell Biology, 57, pp. 40-47. (doi: 10.1016/j.ceb.2018.10.007) (PMID:30453145) (PMCID:PMC7083226)

Mancini, S., Mahmud, Z. A., Jenkins, L. , Bolognini, D., Newman, R., Barnes, M., Edye, M. E., McMahon, S. B., Tobin, A. B. and Milligan, G. (2019) On-target and off-target effects of novel orthosteric and allosteric activators of GPR84. Scientific Reports, 9, 1861. (doi: 10.1038/s41598-019-38539-1) (PMID:30755705) (PMCID:PMC6372602)

Müskens, F. M., Ward, R. J., Herkt, D., van de Langemheen, H., Tobin, A. B. , Liskamp, R. M.J. and Milligan, G. (2019) Design, synthesis and evaluation of a diazirine photoaffinity probe for ligand-based receptor capture targeting G protein-coupled receptors. Molecular Pharmacology, 95(2), pp. 196-209. (doi: 10.1124/mol.118.114249) (PMID:30514721) (PMCID:PMC6324650)

2018

Kennedy, A. J., Ballante, F., Johansson, J. R., Milligan, G. , Sunström, L., Nordqvist, A. and Carlsson, J. (2018) Structural characterization of agonist binding to protease-activated receptor 2 through mutagenesis and computational modeling. ACS Pharmacology and Translational Science, 1(2), pp. 119-133. (doi: 10.1021/acsptsci.8b00019)

Hansen, A. H., Sergeev, E. , Bolognini, D., Sprenger, R. R., Ekberg, J. H., Ejsing, C. S., McKenzie, C. J., Rexen Ulven, E., Milligan, G. and Ulven, T. (2018) Discovery of a potent thiazolidine free fatty acid receptor 2 agonist with favorable pharmacokinetic properties. Journal of Medicinal Chemistry, 61(21), pp. 9534-9550. (doi: 10.1021/acs.jmedchem.8b00855) (PMID:30247908)

Drew, J. E. et al. (2018) Dietary fibers inhibit obesity in mice, but host responses in the cecum and liver appear unrelated to fiber-specific changes in cecal taxonomic composition. Scientific Reports, 8, 15566. (doi: 10.1038/s41598-018-34081-8) (PMID:30349136) (PMCID:PMC6197265)

Divorty, N., Milligan, G. , Graham, D. and Nicklin, S. A. (2018) The orphan receptor GPR35 contributes to angiotensin II–induced hypertension and cardiac dysfunction in mice. American Journal of Hypertension, 31(9), pp. 1049-1058. (doi: 10.1093/ajh/hpy073) (PMID:29860395) (PMCID:PMC6077831)

Marsango, S., Ward, R. J., Alvarez-Curto, E. and Milligan, G. (2018) Muscarinic receptor oligomerization. Neuropharmacology, 136(Part C), pp. 401-410. (doi: 10.1016/j.neuropharm.2017.11.023) (PMID:29146505) (PMCID:PMC6078712)

Binti Mohd Amir, N. A.S., Mackenzie, A. E., Jenkins, L. , Boustani, K., Hillier, M. C., Tsuchiya, T., Milligan, G. and Pease, J. E. (2018) Evidence for the existence of a CXCL17 receptor distinct from GPR35. Journal of Immunology, 201(2), pp. 714-724. (doi: 10.4049/jimmunol.1700884) (PMID:29875152) (PMCID:PMC6036231)

Milligan, G. (2018) G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35. British Journal of Pharmacology, 175(13), pp. 2543-2553. (doi: 10.1111/bph.14042) (PMID:28940377) (PMCID:PMC6003633)

Milligan, G. and Inoue, A. (2018) Genome editing provides new insights into receptor-controlled signalling pathways. Trends in Pharmacological Sciences, 39(5), pp. 481-493. (doi: 10.1016/j.tips.2018.02.005) (PMID:29548548)

Pediani, J. D. , Ward, R. J., Marsango, S. and Milligan, G. (2018) Spatial intensity distribution analysis: studies of G Protein-coupled receptor oligomerization. Trends in Pharmacological Sciences, 39(2), pp. 175-186. (doi: 10.1016/j.tips.2017.09.001) (PMID:29032835) (PMCID:PMC5783713)

Reichardt, N. et al. (2018) Specific substrate-driven changes in human faecal microbiota composition contrast with functional redundancy in short-chain fatty acid production. ISME Journal, 12, pp. 610-622. (doi: 10.1038/ismej.2017.196) (PMID:29192904)

2017

Mahmud, Z. A., Jenkins, L. , Ulven, T., Labéguère, F., Gosmini, R., De Vos, S., Hudson, B. D. , Tikhonova, I. G. and Milligan, G. (2017) Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84. Scientific Reports, 7, 17953. (doi: 10.1038/s41598-017-18159-3) (PMID:29263400) (PMCID:PMC5738391)

Viskaitis, P. et al. (2017) Modulation of SF1 neuron activity coordinately regulates both feeding behaviour and associated emotional states. Cell Reports, 21(12), pp. 3559-3572. (doi: 10.1016/j.celrep.2017.11.089) (PMID:29262334) (PMCID:PMC5746599)

Sergeev, E. , Hansen, A. H., Bolognini, D., Kawakami, K., Kishi, T., Aoki, J., Ulven, T., Inoue, A., Hudson, B. D. and Milligan, G. (2017) A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias. Scientific Reports, 7, 13741. (doi: 10.1038/s41598-017-14096-3) (PMID:29061999) (PMCID:PMC5653858)

Herrick-Davis, K., Milligan, G. and Di Giovanni, G. (Eds.) (2017) G-Protein-Coupled Receptor Dimers. Series: Receptors. Humana Press: Cham. ISBN 9783319601724

Milligan, G. , Alvarez-Curto, E. , Hudson, B. D. , Prihandoko, R. and Tobin, A. B. (2017) FFA4/GPR120: pharmacology and therapeutic opportunities. Trends in Pharmacological Sciences, 38(9), pp. 809-821. (doi: 10.1016/j.tips.2017.06.006) (PMID:28734639) (PMCID:PMC5582618)

Ward, R. J., Marsango, S., Pediani, J. D. and Milligan, G. (2017) The use of spatial intensity distribution analysis to examine G protein-coupled receptor oligomerization. In: Herrick-Davis, K., Milligan, G. and Di Giovanni, G. (eds.) G-Protein-Coupled Receptor Dimers. Series: Receptors (33). Humana Press: Cham, pp. 15-38. ISBN 9783319601724 (doi: 10.1007/978-3-319-60174-8_2)

Prokop, S., Perry, N. A., Vishnivetskiy, S. A., Toth, A. D., Inoue, A., Milligan, G. , Iverson, T. M., Hunyady, L. and Gurevich, V. V. (2017) Differential manipulation of arrestin-3 binding to basal and agonist-activated G protein-coupled receptors. Cellular Signalling, 36, pp. 98-107. (doi: 10.1016/j.cellsig.2017.04.021) (PMID:28461104)

Lopez-Gimenez, J., Alvarez-Curto, E. and Milligan, G. (2017) M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes. Cellular Signalling, 35, pp. 208-222. (doi: 10.1016/j.cellsig.2017.04.006) (PMID:28411124)

Kaspersen, M. H., Jenkins, L. , Dunlop, J. , Milligan, G. and Ulven, T. (2017) Succinct synthesis of saturated hydroxy fatty acids and in vitro evaluation of all hydroxylauric acids on FFA1, FFA4 and GPR84. MedChemComm, 8(6), pp. 1360-1365. (doi: 10.1039/c7md00130d)

Ward, R. J., Pediani, J. D. , Harikumar, K. G., Miller, L. J. and Milligan, G. (2017) Spatial intensity distribution analysis quantifies the extent and regulation of homodimerization of the secretin receptor. Biochemical Journal, 474(11), pp. 1879-1895. (doi: 10.1042/BCJ20170184) (PMID:28424368) (PMCID:PMC5442643)

Watterson, K. R. et al. (2017) Probe-dependent negative allosteric modulators of the long-chain free fatty acid receptor FFA4. Molecular Pharmacology, 91(6), pp. 630-641. (doi: 10.1124/mol.116.107821) (PMID:28385906) (PMCID:PMC5438128)

Marsango, S., Caltabiano, G., Jiménez-Rosés, M., Millan, M. J., Pediani, J. D. , Ward, R. J. and Milligan, G. (2017) A molecular basis for selective antagonist destabilization of dopamine D3 receptor quaternary organization. Scientific Reports, 7, 2134. (doi: 10.1038/s41598-017-02249-3) (PMID:28522847) (PMCID:PMC5437050)

Houthuijzen, J. M. et al. (2017) Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance. FASEB Journal, 31(5), pp. 2195-2209. (doi: 10.1096/fj.201601248R) (PMID:28183801) (PMCID:PMC5388545)

Mackenzie, A. E. and Milligan, G. (2017) The emerging pharmacology and function of GPR35 in the nervous system. Neuropharmacology, 113(part B), pp. 661-671. (doi: 10.1016/j.neuropharm.2015.07.035) (PMID:26232640)

Milligan, G. and Kimura, I. (Eds.) (2017) Free Fatty Acid Receptors. Series: Handbook of experimental pharmacology. Springer International Publishing. ISBN 9783319506920

Hansen, A. H., Sergeev, E. , Pandey, S. K., Hudson, B. D. , Christiansen, E., Milligan, G. and Ulven, T. (2017) Development and characterization of a fluorescent tracer for the free fatty acid receptor 2 (FFA2/GPR43). Journal of Medicinal Chemistry, 60(13), pp. 5638-5645. (doi: 10.1021/acs.jmedchem.7b00338) (PMID:28570808)

Milligan, G. , Bolognini, D. and Sergeev, E. (2017) Ligands at the free fatty acid receptors 2/3 (GPR43/GPR41). In: Milligan, G. and Kimura, I. (eds.) Free Fatty Acid Receptors. Series: Handbook of experimental pharmacology (236). Springer International Publishing, pp. 17-32. ISBN 9783319506920 (doi: 10.1007/164_2016_49)

Milligan, G. , Shimpukade, B., Ulven, T. and Hudson, B. D. (2017) Complex pharmacology of free fatty acid receptors. Chemical Reviews, 117(1), pp. 67-110. (doi: 10.1021/acs.chemrev.6b00056) (PMID:27299848)

2016

Alvarez-Curto, E. , Inoue, A., Jenkins, L. , Raihan, S. Z., Prihandoko, R., Tobin, A. B. and Milligan, G. (2016) Targeted elimination of G proteins and arrestins defines their specific contributions to both intensity and duration of G protein-coupled receptor signalling. Journal of Biological Chemistry, 291(53), pp. 27147-27159. (doi: 10.1074/jbc.M116.754887) (PMID:27852822) (PMCID:PMC5207144)

Azevedo, C. M. G. et al. (2016) Non-acidic free fatty acid receptor 4 agonists with antidiabetic activity. Journal of Medicinal Chemistry, 59(19), pp. 8868-8878. (doi: 10.1021/acs.jmedchem.6b00685)

Bolognini, D. et al. (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. Journal of Biological Chemistry, 291, pp. 18915-18931. (doi: 10.1074/jbc.M116.736157) (PMID:27385588) (PMCID:PMC5009265)

Alvarez-Curto, E. and Milligan, G. (2016) Metabolism meets immunity: the role of free fatty acid receptors in the immune system. Biochemical Pharmacology, 114, pp. 3-13. (doi: 10.1016/j.bcp.2016.03.017) (PMID:27002183)

Pediani, J. D. , Ward, R. J., Godin, A. G., Marsango, S. and Milligan, G. (2016) Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs. Journal of Biological Chemistry, 291, pp. 13132-13146. (doi: 10.1074/jbc.M115.712562) (PMID:27080256) (PMCID:PMC4933229)

Nuber, S., Zabel, U., Lorenz, K., Nuber, A., Milligan, G. , Tobin, A. B. , Lohse, M. J. and Hoffmann, C. (2016) β-Arrestin biosensors reveal a rapid, receptor-dependent activation/deactivation cycle. Nature, 531, pp. 661-664. (doi: 10.1038/nature17198) (PMID:27007855)

Hansen, S. V.F. et al. (2016) Discovery of a potent free fatty acid 1 receptor agonist with low lipophilicity, low polar surface area and robust in vivo efficacy. Journal of Medicinal Chemistry, 59, pp. 2841-2846. (doi: 10.1021/acs.jmedchem.5b01962)

Grundmann, M., Tikhonova, I. G., Hudson, B. D. , Smith, N. J., Mohr, K., Ulven, T., Milligan, G. , Kenakin, T. and Kostenis, E. (2016) A molecular mechanism for sequential activation of a G Protein-coupled receptor. Cell Chemical Biology, 23(3), pp. 392-403. (doi: 10.1016/j.chembiol.2016.02.014) (PMID:26991104)

Bolognini, D., Tobin, A. B. , Milligan, G. and Moss, C. E. (2016) The pharmacology and function of receptors for short-chain fatty acids. Molecular Pharmacology, 89(3), pp. 388-398. (doi: 10.1124/mol.115.102301) (PMID:26719580)

Moreno, J. L. et al. (2016) Allosteric signaling through an mGlu2 and 5-HT2A heteromeric receptor complex and its potential contribution to schizophrenia. Science Signaling, 9(410), ra5. (doi: 10.1126/scisignal.aab0467) (PMID:26758213) (PMCID:PMC4819166)

Sergeev, E. , Hansen, A. H., Pandey, S. K., MacKenzie, A. E., Hudson, B. D. , Ulven, T. and Milligan, G. (2016) Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands. Journal of Biological Chemistry, 291, pp. 303-317. (doi: 10.1074/jbc.M115.687939) (PMID:26518871) (PMCID:PMC4697166)

Christiansen, E., Hudson, B. D. , Hansen, A. H., Milligan, G. and Ulven, T. (2016) Development and characterization of a potent free fatty acid receptor 1 (FFA1) fluorescent tracer. Journal of Medicinal Chemistry, 59(10), pp. 4849-4858. (doi: 10.1021/acs.jmedchem.6b00202) (PMID:27074625)

McCallum, J. E., Mackenzie, A. E., Divorty, N., Clarke, C., Delles, C. , Milligan, G. and Nicklin, S. A. (2016) G protein-coupled receptor 35 mediates human saphenous vein vascular smooth muscle cell migration and endothelial cell proliferation. Journal of Vascular Research, 52(6), pp. 383-395. (doi: 10.1159/000444754) (PMID:27064272) (PMCID:PMC4959467)

Prihandoko, R., Alvarez-Curto, E. , Hudson, B. D. , Butcher, A. J., Ulven, T., Miller, A. M., Tobin, A. B. and Milligan, G. (2016) Distinct phosphorylation clusters determines the signalling outcome of the free fatty acid receptor FFA4/GPR120. Molecular Pharmacology, 89(5), pp. 505-520. (doi: 10.1124/mol.115.101949) (PMID:26873857)

2015

Schrage, R. et al. (2015) The experimental power of FR900359 to study Gq-regulated biological processes. Nature Communications, 6, p. 10156. (doi: 10.1038/ncomms10156) (PMID:26658454) (PMCID:PMC4682109)

Brown, J.H., Catterall, W.A., Conn, P.J., Cull-Candy, S.G., Dingledine, R., Harden, T.K., Insel, P.A., Milligan, G. and Traynelis, S.F. (2015) The first 50 years of molecular pharmacology. Molecular Pharmacology, 88(1), pp. 139-140. (doi: 10.1124/mol.115.099564) (PMID:25943115)

Mckinney, C.A., Kennedy, S. , Baillie, G.S. , Milligan, G. and Nicklin, S.A. (2015) Angiotensin-(1-7) and angiotensin-(1-9) inhibit vascular smooth muscle cell growth and migration in vitro and vascular remodelling in vivo. Atherosclerosis, 241(1), e44. (doi: 10.1016/j.atherosclerosis.2015.04.158)

Milligan, G. , Alvarez-Curto, E. , Watterson, K.R., Ulven, T. and Hudson, B.D. (2015) Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4. British Journal of Pharmacology, 172(13), pp. 3254-3265. (doi: 10.1111/bph.12879) (PMID:25131623)

Marsango, S., Caltabiano, G., Pou, C., Varela Liste, M. J. and Milligan, G. (2015) Analysis of human dopamine D3 receptor quaternary structure. Journal of Biological Chemistry, 290, pp. 15146-15162. (doi: 10.1074/jbc.M114.630681) (PMID:25931118) (PMCID:PMC4463457)

Milligan, G. , Liste, M. J. V., Caltabiano, G. C., Alvarez-Curto, E. and Marsango, S. (2015) Defining the organizational structure of dopamine and muscarninic acetylcholine receptors. SpringerPlus, 4(Sup 1), L7. (doi: 10.1186/2193-1801-4-s1-l7) (PMID:27386224) (PMCID:PMC4796694)

Aslanoglou, D., Alvarez-Curto, E. , Marsango, S. and Milligan, G. (2015) Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers. Journal of Biological Chemistry, 290(23), pp. 14785-14796. (doi: 10.1074/jbc.M115.649079) (PMID:25918156) (PMCID:PMC4505543)

Christiansen, E. et al. (2015) Activity of dietary fatty acids on FFA1 and FFA4 and characterisation of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases. British Journal of Nutrition, 113(11), pp. 1677-1688. (doi: 10.1017/S000711451500118X) (PMID:25916176)

Liste, M. J., Caltabiano, G., Ward, R. J., Alvarez-Curto, E. , Marsango, S. and Milligan, G. (2015) The molecular basis of oligomeric organization of the human m3 muscarinic acetylcholine receptor. Molecular Pharmacology, 87(6), pp. 936-953. (doi: 10.1124/mol.114.096925) (PMID:25769304)

Ward, R. J., Pediani, J. D. , Godin, A. G. and Milligan, G. (2015) Regulation of oligomeric organization of the serotonin 5-hydroxytryptamine 2C (5-HT2C) receptor observed by spatial intensity distribution analysis. Journal of Biological Chemistry, 290(20), pp. 12844-12857. (doi: 10.1074/jbc.M115.644724) (PMID:25825490) (PMCID:PMC4432300)

Alvarez-Curto, E. and Milligan, G. (2015) Defining the functional equivalence of wild-type and chemically engineered G protein-coupled receptors. In: Thiel, G. (ed.) Designer Receptors Exclusively Activated by Designer Drugs. Series: Neuromethods (108). Springer New York, pp. 1-28. ISBN 9781493929436 (doi: 10.1007/978-1-4939-2944-3_1)

Divorty, N., Mackenzie, A., Nicklin, S. and Milligan, G. (2015) G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease. Frontiers in Pharmacology, 6, 41. (doi: 10.3389/fphar.2015.00041) (PMID:25805994) (PMCID:PMC4354270)

Marsango, S., Varela, M. J. and Milligan, G. (2015) Approaches to characterize and quantify oligomerization of GPCRs. In: Filizola, M. (ed.) G Protein-Coupled Receptors in Drug Discovery. Series: Methods in Molecular Biology, 1335 (1335). Springer New York, pp. 95-105. ISBN 9781493929139 (doi: 10.1007/978-1-4939-2914-6_7)

2014

Hudson, B. D. , Christiansen, E., Murdoch, H., Jenkins, L. , Hansen, A. H., Madsen, O., Ulven, T. and Milligan, G. (2014) Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands. Molecular Pharmacology, 86(2), pp. 200-210. (doi: 10.1124/mol.114.093294)

Hudson, B. D. , Shimpukade, B., Milligan, G. and Ulven, T. (2014) The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120). Journal of Biological Chemistry, 289, pp. 20345-20358. (doi: 10.1074/jbc.M114.561449) (PMID:24860101) (PMCID:PMC4106347)

Zakrys, L., Ward, R. J., Pediani, J. D. , Godin, A. G., Graham, G. J. and Milligan, G. (2014) Roundabout 1 exists predominantly as a basal dimeric complex and this is unaffected by binding of the ligand Slit2. Biochemical Journal, 461(1), pp. 61-73. (doi: 10.1042/BJ20140190)

Butcher, A. J., Hudson, B. D. , Shimpukade, B., Alvarez-Curto, E. , Prihandoko, R., Ulven, T., Milligan, G. and Tobin, A. B. (2014) Concomitant action of structural elements and receptor phosphorylation determine arrestin-3 interaction with the free fatty acid receptor FFA4. Journal of Biological Chemistry, 289, pp. 18451-18465. (doi: 10.1074/jbc.M114.568816) (PMID:24817122) (PMCID:PMC4140278)

Fjaere, E. et al. (2014) Indomethacin treatment prevents high fat diet-induced obesity and insulin resistance but not glucose intolerance in C57BL/6J mice. Journal of Biological Chemistry, 289(23), pp. 16032-16045. (doi: 10.1074/jbc.M113.525220)

McKinney, C. A., Fattah, C., Loughrey, C. M. , Milligan, G. and Nicklin, S. A. (2014) Angiotensin-(1-7) and angiotensin-(1-9): function in cardiac and vascular remodeling. Clinical Science, 126, pp. 815-827. (doi: 10.1042/CS20130436)

Milligan, G. , Ulven, T., Murdoch, H. and Hudson, B. D. (2014) G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets. British Journal of Nutrition, 111(S1), S3-S7. (doi: 10.1017/S0007114513002249)

Ferre, S., Casado, V., Devi, L. A., Filizola, M., Jockers, R., Lohse, M. J., Milligan, G. , Pin, J.-P. and Guitart, X. (2014) G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives. Pharmacological Reviews, 66(2), pp. 413-434. (doi: 10.1124/pr.113.008052)

Ward, R.J. and Milligan, G. (2014) Structural and biophysical characterisation of G protein-coupled receptor ligand binding using resonance energy transfer and fluorescent labelling techniques. Biochimica et Biophysica Acta: Biomembranes, 1838(1A), pp. 3-14. (doi: 10.1016/j.bbamem.2013.04.007)

Mackenzie, A.E. et al. (2014) The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat gpr35. Molecular Pharmacology, 85(1), pp. 91-104. (doi: 10.1124/mol.113.089482)

Watterson, K. R., Hudson, B. D. , Ulven, T. and Milligan, G. (2014) Treatment of type 2 diabetes by free fatty acid receptor agonists. Frontiers in Endocrinology, 5, 137. (doi: 10.3389/fendo.2014.00137) (PMID:25221541) (PMCID:PMC4147718)

2013

Horobin, R.W. , Rashid-Doubell, F., Pediani, J.D. and Milligan, G. (2013) Predicting small molecule fluorescent probe localization in living cells using QSAR modeling. 1. Overview and models for probes of structure, properties and function in single cells. Biotechnic and Histochemistry, 88(8), pp. 440-460. (doi: 10.3109/10520295.2013.780634)

Hudson, B.D. , Shimpukade, B., Mackenzie, A.E., Butcher, A.J., Pediani, J.D. , Christiansen, E., Heathcote, H., Tobin, A.B., Ulven, T. and Milligan, G. (2013) The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism. Molecular Pharmacology, 84(5), pp. 710-725. (doi: 10.1124/mol.113.087783)

Perez-Aso, M., Segura, V., Montó, F., Barettino, D., Noguera, M.A., Milligan, G. and D'Ocon, P. (2013) The three α₁-adrenoceptor subtypes show different spatio-temporal mechanisms of internalization and ERK1/2 phosphorylation. Biochimica et Biophysica Acta: Molecular Cell Research, 1833(10), pp. 2322-2333. (doi: 10.1016/j.bbamcr.2013.06.013)

Scott, E., Loya, K., Mountford, J., Milligan, G. and Baker, A. H. (2013) MicroRNA regulation of endothelial homeostasis and commitment—implications for vascular regeneration strategies using stem cell therapies. Free Radical Biology and Medicine, 64, pp. 52-60. (doi: 10.1016/j.freeradbiomed.2013.04.037)

Hudson, B.D. , Murdoch, H. and Milligan, G. (2013) The effects of species ortholog and SNP variation on receptors for free fatty acids. Molecular Endocrinology, 27(8), pp. 1177-1187. (doi: 10.1210/me.2013-1085)

Milligan, G. (2013) The prevalence, maintenance, and relevance of G protein-coupled receptor oligomerization. Molecular Pharmacology, 84(1), pp. 158-169. (doi: 10.1124/mol.113.084780)

Hudson, B.D. et al. (2013) Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor. Journal of Biological Chemistry, 288(24), pp. 17296-17312. (doi: 10.1074/jbc.M113.455337)

Christiansen, E. et al. (2013) Discovery of TUG-770: a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes. ACS Medicinal Chemistry Letters, 4(5), pp. 441-445. (doi: 10.1021/ml4000673)

Neetoo-Isseljee, Z., MacKenzie, A.E., Southern, C., Jerman, J., McIver, E. G., Harries, N., Taylor, D. L. and Milligan, G. (2013) High-throughput identification and characterization of novel, species-selective GPR35 agonists. Journal of Pharmacology and Experimental Therapeutics, 344(3), pp. 568-578. (doi: 10.1124/jpet.112.201798)

Christiansen, E. et al. (2013) Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability. Journal of Medicinal Chemistry, 56(3), pp. 982-992. (doi: 10.1021/jm301470a)

Clarke, C., Flores-Muñoz, M., McKinney, C. A., Milligan, G. and Nicklin, S. A. (2013) Regulation of cardiovascular remodeling by the counter-regulatory axis of the renin–angiotensin system. Future Cardiology, 9(1), pp. 23-38. (doi: 10.2217/fca.12.75)

Howard, L., MacKenzie, R. M., Pchelintsev, N. A., McBryan, T., McClure, J. D. , McBride, M. W. , Kane, N. M., Adams, P. D., Milligan, G. and Baker, A. H. (2013) Profiling of transcriptional and epigenetic changes during directed endothelial differentiation of human embryonic stem cells identifies FOXA2 as a marker of early mesoderm commitment. Stem Cell Research and Therapy, 4(2), Art. 36. (doi: 10.1186/scrt192)

Hudson, B. D. , Ulven, T. and Milligan, G. (2013) The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs. Current Topics in Medicinal Chemistry, 13(1), pp. 14-25. (doi: 10.2174/1568026611313010004)

Jenkins, L. , Harries, N., Lappin, J.E., MacKenzie, A.E., Neetoo-Isseljee, Z., Southern, C., McIver, E.G., Nicklin, S.A. , Taylor, D.L. and Milligan, G. (2013) Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. Journal of Pharmacology and Experimental Therapeutics, 343(3), pp. 683-695. (doi: 10.1124/jpet.112.198945) (PMID:22967846) (PMCID:PMC3500541)

Mackenzie, A. E., Neetoo-Isseljee, Z., Southern, C., Jerman, J., McIver, E. G., Hudson, B. D. , Taylor, D. L. and Milligan, G. (2013) Novel and potent GPR35 agonists aid identification of residues important in ligand interaction. FASEB Journal, 27, 655.1.

Patowary, S., Alvarez-Curto, E. , Xu, T.-R., Holz, J.D., Oliver, J.A., Milligan, G. and Raicu, V. (2013) The muscarinic M3acetylcholine receptor exists as two differently sized complexes at the plasma membrane. Biochemical Journal, 452(2), pp. 303-312. (doi: 10.1042/BJ20121902) (PMID:23521066)

Segura, V., Pérez-Aso, M., Montó, F., Carceller, E., Noguera, M.A., Pediani, J. , Milligan, G. , McGrath, I.C. and D’Ocon, P. (2013) Differences in the signaling pathways of α1A- and α1B-adrenoceptors are related to different endosomal targeting. PLoS ONE, 8(5), e64996. (doi: 10.1371/journal.pone.0064996) (PMID:23717684) (PMCID:PMC3663791)

Ward, R.W., Xu, T.-X. and Milligan, G. (2013) GPCR oligomerization and receptor trafficking. Methods in Enzymology, 521, pp. 69-90. (doi: 10.1016/B978-0-12-391862-8.00004-1)

2012

Moreno, J.L. et al. (2012) Identification of three residues essential for 5-hydroxytryptamine 2A-metabotropic glutamate 2 (5-HT2A{middle dot}mGlu2) receptor heteromerization and its psychoactive behavioral function. Journal of Biological Chemistry, 287(53), pp. 44301-44319. (doi: 10.1074/jbc.M112.413161)

Hudson, B. , Christiansen, E., Tikhonova, I.G., Grundmann, M., Kostenis, E., Adams, D.R., Ulven, T. and Milligan, G. (2012) Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs. FASEB Journal, 26(12), pp. 4951-4965. (doi: 10.1096/fj.12-213314)

Hudson, B.D. , Tikhonova, I.G., Pandey, S.K., Ulven, T. and Milligan, G. (2012) Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3. Journal of Biological Chemistry, 287(49), pp. 41195-41209. (doi: 10.1074/jbc.M112.396259)

Christiansen, E. et al. (2012) Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. Journal of Medicinal Chemistry, 55(14), pp. 6624-6628. (doi: 10.1021/jm3002026)

Cunningham, M. R., McIntosh, K. A., Pediani, J. D. , Robben, J., Cooke, A. E., Nilsson, M., Gould, G. W. , Mundell, S., Milligan, G. and Plevin, R. (2012) Novel role for proteinase-activated receptor 2 (PAR2) in membrane trafficking of proteinase-activated receptor 4 (PAR4). Journal of Biological Chemistry, 287(20), pp. 16656-16669. (doi: 10.1074/jbc.M111.315911)

Shimpukade, B., Hudson, B.D. , Hogaard, C.K., Milligan, G. and Ulven, T. (2012) Discovery of a potent and selective GPR120 agonist. Journal of Medicinal Chemistry, 55(9), pp. 4511-4515. (doi: 10.1021/jm300215x)

Xu, T.-R., Ward, R. J., Pediani, J. D. and Milligan, G. (2012) Intramolecular fluorescence resonance energy transfer (FRET) sensors of the orexin OX1 and OX2 receptors identify slow kinetics of agonist activation. Journal of Biological Chemistry, 287, pp. 14937-14949. (doi: 10.1074/jbc.M111.334300)

Kane, N. M. et al. (2012) Role of MicroRNAs 99b, 181a, and 181b in the differentiation of human embryonic stem cells to vascular endothelial cells. Stem Cells, 30(4), pp. 643-654. (doi: 10.1002/stem.1026)

White, K., Kane, N. M., Milligan, G. and Baker, A. H. (2012) The role of miRNA in stem cell pluripotency and commitment to the vascular endothelial lineage. Microcirculation, 19(3), pp. 196-207. (doi: 10.1111/j.1549-8719.2012.00161.x)

Xu, T.-R., Lu, R.-F., Romano, D., Pitt, A., Houslay, M. D., Milligan, G. and Kolch, W. (2012) Eukaryotic translation initiation factor 3, subunit a, regulates the extracellular signal-regulated kinase pathway. Molecular and Cellular Biology, 32(1), pp. 88-95. (doi: 10.1128/​MCB.05770-11)

Flores, M., Graham, D. , Dominiczak, A.F. , Milligan, G. , Baker, A.H. and Nicklin, S.A. (2012) Angiotensin-(1-9) antagonises Angiotensin II-induced cardiac remodeling via the angiotensin type 2 receptor. Proceedings of the Physiological Society, 27, C1.

Flores, M., Graham, D. , Dominiczak, A. F. , Milligan, G. , Baker, A. H. and Nicklin, S. A. (2012) Abstract 231: angiotensin-(1-9) antagonises cardiac remodelling in a mouse model of Angiotensin Ii-induced hypertension. Hypertension, 60, A231.

Georgoussi, Z., Georganta, E.M. and Milligan, G. (2012) The other side of opioid receptor signalling: regulation by protein-protein interaction. Current Drug Targets, 13(1), pp. 80-102. (doi: 10.2174/138945012798868470)

Laarman, A.J. et al. (2012) Staphylococcus aureus Staphopain A inhibits CXCR2-dependent neutrophil activation and chemotaxis. EMBO Journal, 31(17), pp. 3607-3619. (doi: 10.1038/emboj.2012.212)

Pou, C., Mannoury la Cour, C., Stoddart, L.A., Millan, M.J. and Milligan, G. (2012) Functional homomers and heteromers of dopamine D_2L and D₃ receptors co-exist at the cell surface. Journal of Biological Chemistry, 287(12), pp. 8864-8878. (doi: 10.1074/jbc.M111.326678)

Terhzaz, S. , Cabrero, P. , Robben, J.H., Radford, J.C., Hudson, B.D. , Milligan, G. , Dow, J.A.T. and Davies, S.A. (2012) Mechanism and function of drosophila capa GPCR: a desiccation stress-responsive receptor with functional homology to human neuromedinU receptor. PLoS ONE, 7(1), e29897. (doi: 10.1371/journal.pone.0029897) (PMID:22253819) (PMCID:PMC3256212)

2011

Mackenzie, A.E., Lappin, J.E., Taylor, D.L., Nicklin, S.A. and Milligan, G. (2011) GPR35 as a novel therapeutic target. Frontiers in Endocrinology, 2, 68. (doi: 10.3389/fendo.2011.00068) (PMID:22654822) (PMCID:PMC3356001)

Alvarez-Curto, E. , Prihandoko, R., Tautermann, C. S., Zwier, J. M., Pediani, J. D. , Lohse, M. J., Hoffmann, C., Tobin, A. B. and Milligan, G. (2011) Developing chemical genetic approaches to explore G protein-coupled receptor function: validation of the use of a Receptor Activated Solely by Synthetic Ligand (RASSL). Molecular Pharmacology, 80(6), pp. 1033-1046. (doi: 10.1124/mol.111.074674) (PMID:21880827) (PMCID:PMC3228535)

Ward, R. J., Pediani, J. D. and Milligan, G. (2011) Heteromultimerization of cannabinoid CB₁ receptor and orexin OX₁ receptor generates a unique complex in which both protomers are regulated by orexin A. Journal of Biological Chemistry, 286(43), pp. 37414-37428. (doi: 10.1074/jbc.M111.287649)

Howard, L., Kane, N., Milligan, G. and Baker, A. H. (2011) MicroRNAs regulating cell pluripotency and vascular differentiation. Vascular Pharmacology, 55(4), pp. 69-78. (doi: 10.1016/j.vph.2011.08.002)

Xu, T.‑R., Ward, R. J., Pediani, J. D. and Milligan, G. (2011) The orexin OX₁ receptor exists predominantly as a homodimer in the basal state: potential regulation of receptor organization by both agonist and antagonist ligands. Biochemical Journal, 439(1), pp. 171-183. (doi: 10.1042/BJ20110230)

Van Lith, M., Tiwari, S., Pediani, J. , Milligan, G. and Bulleid, N. J. (2011) Real-time monitoring of redox changes in the mammalian endoplasmic reticulum. Journal of Cell Science, 124(14), pp. 2349-2356. (doi: 10.1242/jcs.085530)

Smith, N.J. et al. (2011) Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. Molecular Pharmacology, 80(1), pp. 163-173. (doi: 10.1124/mol.110.070789)

Nejsum, L.N., Christensen, T.M., Robben, J.H., Milligan, G. , Deen, P.M.T., Bichet, D.G. and Levin, K. (2011) Novel mutation in the AVPR2 gene in a Danish male with nephrogenic diabetes insipidus caused by ER retention and subsequent lysosomal degradation of the mutant receptor. NDT Plus, 4(3), pp. 158-163. (doi: 10.1093/ndtplus/sfr010) (PMID:21629670) (PMCID:PMC3103721)

Schmidt, J. et al. (2011) Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. Journal of Biological Chemistry, 286(12), pp. 10628-10640. (doi: 10.1074/jbc.M110.210872)

Anthony, D.F., Sin, Y.Y. , Vadrevu, S., Advant, N., Day, J.P., Byrne, A.M., Lynch, M.J., Milligan, G. , Houslay, M.D. and Baillie, G.S. (2011) β-Arrestin 1 inhibits the GAP function of ARHGAP21 so as to promote the activation of RhoA following angiotensin II type 1A receptor stimulation. Molecular and Cellular Biology, 31(5), pp. 1066-1075. (doi: 10.1128/MCB.00883-10) (PMID:21173159) (PMCID:PMC3067824)

Ward, R. J., Pediani, J. D. and Milligan, G. (2011) Ligand-induced internalisation of the orexin OX1 and cannabinoid CB1 receptors assessed via N-terminal SNAP and CLIP-tagging. British Journal of Pharmacology, 162(6), pp. 1439-1452. (doi: 10.1111/j.1476-5381.2010.01156.x)

Flores-Munoz, M., Smith, N. J., Haggerty, C., Milligan, G. and Nicklin, S. A. (2011) Angiotensin1-9 antagonises pro-hypertrophic signalling in cardiomyocytes via the angiotensin type 2 receptor. Journal of Physiology, 589(4), pp. 939-951. (doi: 10.1113/jphysiol.2010.203075)

Smith, N.J., Bennett, K. and Milligan, G. (2011) When simple agonism is not enough: Emerging modalities of GPCR ligands. Molecular and Cellular Endocrinology, 331(2), pp. 241-247. (doi: 10.1016/j.mce.2010.07.009)

Dimond, P. et al. (2011) G protein-coupled receptor modulation with pepducins: moving closer to the clinic. Annals of the New York Academy of Sciences, 1226(1), pp. 34-49. (doi: 10.1111/j.1749-6632.2011.06039.x)

Hudson, B.D. , Smith, N.J. and Milligan, G. (2011) Experimental challenges to targeting poorly characterized GPCRs: uncovering the therapeutic potential for free fatty acid receptors. In: Neubig, R.R. (ed.) Pharmacology of G Protein Coupled Receptors. Series: Advances in Pharmacology (62). Elsevier Academic Press: Amsterdam, The Netherlands, pp. 175-218. ISBN 9780123859525 (doi: 10.1016/B978-0-12-385952-5.00006-3)

Milligan, G. (2011) Orthologue selectivity and ligand bias: translating the pharmacology of GPR35. Trends in Pharmacological Sciences, 32(5), pp. 317-325. (doi: 10.1016/j.tips.2011.02.002)

MX PA/A/2005/012546 (2011) Materials and Methods Relating to G-Protein Coupled Oligomers. .

US 10/555,709 (2011) Materials and Methods Relating to G-Protein Coupled Receptor Oligomers. .

US 12/119,401 (2011) Materials and Methods Relating to G-Protein Coupled Receptor Oligomers. .

CN 200480017258.7 (2011) Materials and Methods Relating to G-Protein Coupled Receptor Oligomers. .

TW 093114280 (2011) Materials and Methods Relating to G-Protein Coupled Receptor Oligomers. .

US 09/913, 762 (2011) Receptor Assay. .

Saenz del Burgo, L. and Milligan, G. (2011) Ligand regulation of GPCR quaternary structure. In: Giraldo, J. and Pin, J.-P. (eds.) G Protein-Coupled Receptors: From Structure to Function G Protein-Coupled Receptors: From Structure to Function. Series: RSC drug discovery (8). RSC Publishing: Cambridge, UK, pp. 111-152. ISBN 9781849733441 (doi: 10.1039/9781849733441-00111)

Schröder, R. et al. (2011) Applying label-free dynamic mass redistribution technology to frame signaling of G protein–coupled receptors noninvasively in living cells. Nature Protocols, 6(11), pp. 1748-1760. (doi: 10.1038/nprot.2011.386)

Tarrasón, G. et al. (2011) The sphingosine-1-phosphate receptor-1 antagonist, W146, causes early and short-lasting peripheral blood lymphopenia in mice. International Immunopharmacology, 11(11), pp. 1773-1779. (doi: 10.1016/j.intimp.2011.07.004)

Ward, R.J., Alvarez-Curto, E. and Milligan, G. (2011) Using the Flp-In™ T-Rex™ System to Regulate GPCR Expression. Methods in Molecular Biology, 746, pp. 21-37. (doi: 10.1007/978-1-61779-126-0_2)

2010

Burton, P. et al. (2010) Erythro-9-(2-hydroxy-3-nonyl)adenine (EHNA) blocks differentiation and maintains the expression of pluripotency markers in human embryonic stem cells. Biochemical Journal, 432(3), pp. 575-584. (doi: 10.1042/BJ20100726)

Kane, N. M. et al. (2010) Lentivirus-mediated reprogramming of somatic cells in the absence of transgenic transcription factors. Molecular Therapy, 18(12), pp. 2139-2145. (doi: 10.1038/mt.2010.231)

Smith, N. J. and Milligan, G. (2010) Allostery at G protein-coupled receptor Homo- and Heteromers: uncharted pharmacological landscapes. Pharmacological Reviews, 62(4), pp. 701-725. (doi: 10.1124/pr.110.002667) (PMID:21079041) (PMCID:PMC2993260)

Lopez-Gimenez, J.F. and Milligan, G. (2010) Opioid regulation of Mu receptor internalisation: relevance to the development of tolerance and dependence. CNS and Neurological Disorders: Drug Targets, 9(5), pp. 616-626. (doi: 10.2174/187152710793361522) (PMID:20632966)

Alvarez-Curto, E. , Pediani, J. D. and Milligan, G. (2010) Applications of fluorescence and bioluminescence resonance energy transfer to drug discovery at G protein coupled receptors. Analytical and Bioanalytical Chemistry, 398(1), pp. 167-180. (doi: 10.1007/s00216-010-3823-4) (PMID:20517598)

Schroder, R. et al. (2010) Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements. Nature Biotechnology, 28(9), pp. 943-949. (doi: 10.1038/nbt.1671)

Burton, P. et al. (2010) Identification and characterization of small-molecule ligands that maintain pluripotency of human embryonic stem cells. Biochemical Society Transactions, 38(4), pp. 1058-1061. (doi: 10.1042/BST0381058)

Alvarez-Curto, E., Ward, R. J., Pediani, J. D. and Milligan, G. (2010) Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogenous time-resolved FRET. Journal of Biological Chemistry, 285(30), pp. 23318-23330. (doi: 10.1074/jbc.M110.122184) (PMID:20489201) (PMCID:PMC2906324)

Khelashvili, G. et al. (2010) GPCR-OKB: the G protein coupled receptor oligomer knowledge base. Bioinformatics, 26(14), pp. 1804-1805. (doi: 10.1093/bioinformatics/btq264)

Kane, N. M., Meloni, M., Spencer, H. L., Craig, M. A., Strehl, R., Milligan, G., Houslay, M. D., Mountford, J. C., Emanueli, C. and Baker, A. H. (2010) Derivation of endothelial cells from human embryonic stem cells by directed differentiation: analysis of microRNA and angiogenesis in vitro and in vivo. Arteriosclerosis, Thrombosis, and Vascular Biology, 30(7), pp. 1389-1397. (doi: 10.1161/ATVBAHA.110.204800)

del Burgo, L. S. and Milligan, G. (2010) Heterodimerisation of G protein-coupled receptors: implications for drug design and ligand screening. Expert Opinion on Drug Discovery, 5(5), pp. 461-474. (doi: 10.1517/17460441003720467) (PMID:22823130)

PA/A/2005/012546 (2010) Materials and Methods Relating to G-Protein Coupled Receptor Oligomers. .

Milligan, G. (2010) The role of dimerisation in the cellular trafficking of G-protein-coupled receptors. Current Opinion in Pharmacology, 10(1), pp. 23-29. (doi: 10.1016/j.coph.2009.09.010) (PMID:19850521)

Andrews, P. et al. (2010) High content screening of feeder-free human embryonic stem cells to identify pro-survival small molecules. Biochemical Journal, 432(Pt 1), pp. 21-33. (doi: 10.1042/BJ20101022)

Burton, P. et al. (2010) Identification and characterization of small-molecule ligands that maintain pluripotency of human embryonic stem cells. Biochemical Society Transactions, 38(4), pp. 1058-1061. (doi: 10.1042/BST0381058)

Jenkins, L. , Alvarez-Curto, E. , Campbell, K., De Munnik, S., Canals Buj, M., Schlyer, S. and Milligan, G. (2010) Agonist activation of the G protein-coupled receptor GPR35 involves transmembrane domain III and is transduced via Gα13 and β-arrestin-2. British Journal of Pharmacology, 162(3), pp. 733-748. (doi: 10.1111/j.1476-5381.2010.01082.x)

Jenkins, L. , Brea, J., Smith, N.J., Hudson, B.D. , Reilly, G., Bryant, N.J., Castro, M., Loza, M.I. and Milligan, G. (2010) Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13. Biochemical Journal, 432(3), pp. 451-459. (doi: 10.1042/BJ20101287)

Stoddart, L.A. and Milligan, G. (2010) Constitutive activity of GPR40/FFA1 intrinsic or assay dependent? Methods in Enzymology, 484, pp. 569-590. (doi: 10.1016/B978-0-12-381298-8.00028-9) (PMID:21036251)

Xu, T. et al. (2010) Inferring signaling pathway topologies from multiple perturbation measurements of specific biochemical species. Science Signaling, 3(113), ra20. (doi: 10.1126/scisignal.2000517)

2009

Robben, J.H., Fenton, R.A., Vargas, S.L., Schweer, H., Peti-Peterdi, J., Deen, P.M.T. and Milligan, G. (2009) Localization of the succinate receptor in the distal nephron and its signaling in polarized MDCK cells. Kidney International, 76(12), pp. 1258-1267. (doi: 10.1038/ki.2009.360)

Milligan, G. (2009) G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function. British Journal of Pharmacology, 158(1), pp. 5-14. (doi: 10.1111/j.1476-5381.2009.00169.x) (PMID:19309353) (PMCID:PMC2795239)

Milligan, G. and McGrath, J.C. (2009) GPCR theme editorial. British Journal of Pharmacology, 158(1), pp. 1-4. (doi: 10.1111/j.1476-5381.2009.00422.x)

Robben, J.H., Kortenoeven, M.L.A., Sze, M., Yae, C., Milligan, G. , Oorschot, V.M., Klumperman, J., Knoers, N.V.A.M. and Deen, P.M.T. (2009) Intracellular activation of vasopressin V2 receptor mutants in nephrogenic diabetes insipidus by nonpeptide agonists. Proceedings of the National Academy of Sciences of the United States of America, 106(29), pp. 12195-12200. (doi: 10.1073/pnas.0900130106)

Smith, N.J., Stoddart, L.A., Devine, N.M., Jenkins, L. and Milligan, G. (2009) The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1. Journal of Biological Chemistry, 284(26), pp. 17527-17539. (doi: 10.1074/jbc.M109.012849) (PMID:19398560) (PMCID:PMC2719392)

Idris, A.I., Sophocleous, A., Landao-Bassonga, E., Merkouris, M., Milligan, G., Baker, D., van't Hof, R.J. and Ralston, S.H. (2009) Cannabinoid receptor type 1 protects against age-related bone loss by regulating osteoblast and adipocyte differentiation of bone marrow stromal cells. Bone, 44(Supple), S222. (doi: 10.1016/j.bone.2009.03.067)

Ward, R. J., Jenkins, L. and Milligan, G. (2009) Selectivity and functional consequences of interactions of family A G protein-coupled receptors with neurochondrin and periplakin. Journal of Neurochemistry, 109(1), pp. 182-192. (doi: 10.1111/j.1471-4159.2009.05918.x)

Ferre, S. et al. (2009) Building a new conceptual framework for receptor heteromers. Nature Chemical Biology, 5(3), pp. 131-134. (doi: 10.1038/nchembio0309-131)

Canals, M., Lopez-Gimenez, J. F. and Milligan, G. (2009) Cell surface delivery and structural re-organization by pharmacological chaperones of an oligomerization-defective α_1b-adrenoceptor mutant demonstrates membrane targeting of GPCR oligomers. Biochemical Journal, 417(1), pp. 161-172. (doi: 10.1042/BJ20081227)

Appelbe, S. and Milligan, G. (2009) Hetero‐Oligomerization of Chemokine Receptors. In: Chemokines, Part B. Series: Methods in Enzymology., 461. Academic Press, pp. 207-225. ISBN 9780123749079 (doi: 10.1016/S0076-6879(09)05410-X)

Bennett, K.A., Langmead, C.J., Wise, A. and Milligan, G. (2009) Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein G{alpha}o1 by the ghrelin receptor. Molecular Pharmacology, 76(4), pp. 802-811. (doi: 10.1124/mol.109.056101)

Brea, J.H. et al. (2009) Evidence for distinct antagonist-revealed functional states of 5-HT_2A receptor homodimers. Molecular Pharmacology, 75(6), pp. 1380-1391. (doi: 10.1124/mol.108.054395)

Idris, A. I., Sophocleous, A., Landa-Bassonga, E., Canals, M., Milligan, G., Baker, D., van't Hof, R. J. and Ralston, S. (2009) Cannabinoid receptor type 1 protects against age-related bone loss by regulating osteoblast and adipocyte differentiation of bone marrow stromal cells. Cell Metabolism, 10(2), pp. 139-147. (doi: 10.1016/j.cmet.2009.07.006)

Milligan, G., Stoddart, L.A. and Smith, N.J. (2009) Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3. British Journal of Pharmacology, 158(1), pp. 146-153. (doi: 10.1111/j.1476-5381.2009.00421.x) (PMID:19719777) (PMCID:PMC2795255)

2008

Lopez-Gimenez, J. F., Vilaro, M. T. and Milligan, G. (2008) Morphine desensitization, internalization and down-regulation of the μ opioid receptor is facilitated by serotonin 5-hydroxytryptamine_2A receptor co-activation. Molecular Pharmacology, 74(5), pp. 1278-1291. (doi: 10.1124/mol.108.048272) (PMID:18703670)

10/555709 (2008) Materials and Methods Relating to G-Protein Coupled Receptor Oligomers. .

Xu, T.-R., Baillie, G. S. , Bhari, N., Houslay, T. M., Pitt, A. M., Adams, D. R., Kolch, W., Houslay, M. D. and Milligan, G. (2008) Mutations of β-arrestin 2 that limit self-association also interfere with interactions with the β₂-adrenoceptor and the ERK1/2 MAPKs: implications for β₂-adrenoceptor signalling via the ERK1/2 MAPKs. Biochemical Journal, 413(1), pp. 51-60. (doi: 10.1042/BJ20080685)

Canals Buj, M. and Milligan, G. (2008) Constitutive activity of the cannabinoid CB1 receptor regulates the function of co-expressed Mu opioid receptors. Journal of Biological Chemistry, 283(17), pp. 11424-11434. (doi: 10.1074/jbc.M710300200)

González-Maeso, J. et al. (2008) Identification of a serotonin/glutamate receptor complex implicated in psychosis. Nature, 452(7183), pp. 93-97. (doi: 10.1038/nature06612)

Milligan, G. (2008) A day in the life of a G protein-coupled receptor: the contribution to function of G protein-coupled receptor dimerization. British Journal of Pharmacology, 153(.), S216-S229. (doi: 10.1038/sj.bjp.0707490)

Hill, C., Brownlie, Z., Davey, J., Milligan, G. and Ladds, G. (2008) Isolation and characterization of a novel human RGS mutant displaying gain-of-function activity. Cellular Signalling, 20(2), pp. 323-336. (doi: 10.1016/j.cellsig.2007.10.016) (PMID:18031991)

Lane, J.R., Henderson, D., Powney, B., Wise, A., Rees, S., Daniels, D., Plumpton, C., Kinghorn, I. and Milligan, G. (2008) Antibodies that identify only the active conformation of G_i family G protein α subunits. FASEB Journal, 22, pp. 1924-1932. (doi: 10.1096/fj.07-100388)

Lane, J.R., Powney, B., Wise, A., Rees, S. and Milligan, G. (2008) G protein-coupling and ligand selectivity of the D_2L and D₃ dopamine receptors. Journal of Pharmacology and Experimental Therapeutics, 325(1), pp. 319-330. (doi: 10.1124/jpet.107.134296)

McCulloch, C., Morrow, V., Milasta, S., Comerford, I., Milligan, G. , Graham, G. , Isaacs, N. and Nibbs, R. (2008) Multiple roles for the C-terminal tail of the chemokine scavenger D6. Journal of Biological Chemistry, 283(12), pp. 7972-7982. (doi: 10.1074/jbc.M710128200)

Noubade, R., Saligrama, N., Spach, K., del Rio, R., Blankenhorn, E.P., Kantidakis, T., Milligan, G. , Rincon, M. and Teuscher, C. (2008) Autoimmune disease-associated histamine receptor H1 alleles exhibit differential protein trafficking and cell surface expression. Journal of Immunology, 180(11), pp. 7471-7479.

Parenty, G., Applebe, S. and Milligan, G. (2008) CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2-DOP receptor hetero-dimer. Biochemical Journal, 412(Pt2), pp. 215-256. (doi: 10.1042/BJ20071689)

Stoddart, L. A., Smith, N. J., Jenkins, L. , Brown, A. J. and Milligan, G. (2008) Conserved Polar Residues in Transmembrane Domains V, VI, and VII of Free Fatty Acid Receptor 2 and Free Fatty Acid Receptor 3 Are Required for the Binding and Function of Short Chain Fatty Acids. Journal of Biological Chemistry, 283(47), pp. 32913-32924. (doi: 10.1074/jbc.M805601200) (PMID:18801738)

Stoddart, L. A., Smith, N. J. and Milligan, G. (2008) International Union of Pharmacology. LXXI. Free Fatty Acid Receptors FFA1, -2, and -3: Pharmacology and Pathophysiological Functions. Pharmacological Reviews, 60(4), pp. 405-417. (doi: 10.1124/pr.108.00802)[Book Review]

2007

Snook, L.A., Milligan, G. , Kieffer, B.L. and Massotte, D. (2007) Co-expression of mu and delta opioid receptors as receptor-G protein fusions enhances both mu and delta signalling via distinct mechanisms. Journal of Neurochemistry, 105(3), pp. 865-873. (doi: 10.1111/j.1471-4159.2008.05215.x)

Noubade, R., Milligan, G. , Zachary, J.F., Blankenhorn, E.P., del Rio, R., Rincorn, M. and Teuscher, C. (2007) Histamine receptor H1 is required for TCR-mediated p38 MAPK activation and optimal IFN-γ production in mice. Journal of Clinical Investigation, 117(11), pp. 3507-3518.

Baillie, G.S. et al. (2007) Mapping binding sites for the PDE4D5 cAMP-specific phosphodiesterase to the N- and C-domains of beta-arrestin using spot-immobilized peptide arrays. Biochemical Journal, 404(1), pp. 71-80. (doi: 10.1042%2FBJ20070005)

Skrabanek, L. et al. (2007) Requirements and ontology for a G protein-coupled receptor oligomerization knowledge base. BMC Bioinformatics, 8(177), (doi: 10.1186/1471-2105-8-177)

Lopez-Gimenez, J. F., Canals Buj, M., Pediani, J. D. and Milligan, G. (2007) The 1b-adrenoceptor exists as a higher-order oligomer: effective oligomerization is required for receptor maturation, surface delivery, and function. Molecular Pharmacology, 71(4), pp. 1015-1029. (doi: 10.1124/mol.106.033035)

Milligan, G. (2007) G protein-coupled receptor dimerisation: molecular basis and relevance to function. Biochimica et Biophysica Acta: Biomembranes, 1768(4), pp. 825-835. (doi: 10.1016/j.bbamem.2006.09.021)

Pin, J.P. et al. (2007) International union of basic and clinical pharmacology. LXVII. Recommendations for the recognition and nomenclature of g protein-coupled receptor heteromultimers. Pharmacological Reviews, 59(1), pp. 5-13. (doi: 10.1124/pr.59.1.5)

Bouvier, M., Heveker, N., Jockers, R., Marullo, S. and Milligan, G. (2007) BRET analysis of GPCR oligomerization: newer does not mean better. Nature Methods, 4(1), pp. 3-4. (doi: 10.1038/nmeth0107-3)

Fredholm, B., Hokfelt, T. and Milligan, G. (2007) G-protein-coupled receptors: an update. Acta Physiologica, 190, pp. 3-7. (doi: 10.1111/j.1748-1716.2007.01689.x)

Jameson, E., Pei, J., Wade, S., Neubig, R., Milligan, G. and Kennedy, R. (2007) Capillary electrophoresis assay for G protein-coupled receptor-mediated GTPase activity. Analytical Chemistry, 79, pp. 1158-1163. (doi: 10.1021/ac061099g)

Lane, J., Powney, B., Wise, A., Rees, S. and Milligan, G. (2007) Protean agonism at the dopamine D-2 receptor: (S)-3-(3-hydroxyphenyl)-N-propylpiperidine is an agonist for activation of G(o1) but an antagonist/inverse agonist for G(i1), G(i2), and G(i3). Molecular Pharmacology, 71, pp. 1349-1359. (doi: 10.1124/mol.106.032722)

Milligan, G. (2007) Allosteric modulation of heterodimeric G-protein-coupled receptors. Trends in Pharmacological Sciences, 28(12), pp. 615-620. (doi: 10.1016/j.tips.2007.11.001)

Milligan, G. , Parenty, G., Stoddart, L. and Lane, J. (2007) Novel pharmacological applications of G-protein-coupled receptor-G protein fusions. Current Opinion in Pharmacology, 7, pp. 521-526. (doi: 10.1016/j.coph.2007.06.007)

Milligan, G. and Vanderbauwhede, W. (2007) Implementation of finite state machines on a reconfigurable device. In: Arslan, T. (ed.) Second NASA/ESA Conference on Adaptive Hardware and Systems (AHS 2007), 5-8 Aug. 2007, Edinburgh, UK. IEEE Computer Society: Los Alamitos, USA, pp. 386-396. ISBN 9780769528663 (doi: 10.1109/AHS.2007.64)

Noubade, R., Milligan, G. , Zachary, J., Blankenhorn, E., del Rio, R., Rincon, M. and Teuscherl, C. (2007) Histamine receptor H-1 is-required for TCR-mediated p38 MAPK activation and optimal IFN-gamma production in mice. Journal of Clinical Investigation, 117, pp. 3507-3518. (doi: 10.1172/JC132792)

Orth, J., Lang, S., Preuss, I., Milligan, G. and Aktories, K. (2007) Action of Pasteurella multocida toxin on G alpha(q) is persistent and independent of interaction with G-protein-coupled receptors. Cellular Signalling, 19, pp. 2174-2182. (doi: 10.1016/j.cellsig.2007.06.016)

Sartania, N. , Appelbe, S., Pediani, J. D. and Milligan, G. (2007) Agonist occupancy of a single monomeric element is sufficient to cause internalization of the dimeric beta(2)-adrenoceptor. Cellular Signalling, 19, pp. 1928-1938. (doi: 10.1016/j.cellsig.2007.05.002)

Stoddart, L., Brown, A. and Milligan, G. (2007) Uncovering the pharmacology of the G protein-coupled receptor GPR40: High apparent constitutive activity in guanosine 5'-O-(3-[S-35] thio) triphosphate binding studies reflects binding of an endogenous agonist. Molecular Pharmacology, 71, pp. 994-1005. (doi: 10.1124/mol.106.031534)

2006

Ellis, J., Pediani, J.D. , Canals Buj, M., Milasta, S. and Milligan, G. (2006) Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. Journal of Biological Chemistry, 281(25), pp. 38812-38824. (doi: 10.1074/jbc.M602494200)

Comerford, I., Milasta, S., Morrow, V., Milligan, G. and Nibbs, R. (2006) The chemokine receptor CCX-CKR mediates effective scavenging of CCL19 in vitro. European Journal of Immunology, 36(7), pp. 1904-1916. (doi: 10.1002/eji.200535716)

Batenburg, W. et al. (2006) Carvedilol-induced antagonism of angiotensin II: a matter of alpha(1)-adrenoceptor blockade. Journal of Hypertension, 24, pp. 1355-1363.

Canals, M., Jenkins, L., Kellett, E. and Milligan, G. (2006) Up-regulation of the angiotensin II type 1 receptor by the MAS proto-oncogene is due to constitutive activation of G(q)/G(11) by MAS. Journal of Biological Chemistry, 281, pp. 16757-16767. (doi: 10.1074/jbc.M601121200)

Ciruela, F. et al. (2006) Presynaptic control of striatal glutamatergic neurotransmission by adenosine A(1)-A(2A) receptor heteromers. Journal of Neuroscience, 26, pp. 2080-2087. (doi: 10.1523/JNEUROSCI.3574-05.2006)

Francke, F., Ward, R., Jenkins, L., Kellett, E., Richter, D., Milligan, G. and Bachner, D. (2006) Interaction of neurochondrin with the melanin-concentrating hormone receptor 1 interferes with G protein-coupled signal transduction but not agonist-mediated internalization. Journal of Biological Chemistry, 281, pp. 32496-32507. (doi: 10.1074/jbc.M602889200)

Milasta, S., Pediani, J., Appelbe, S., Trim, S., Wyatt, M., Cox, P., Fidock, M. and Milligan, G. (2006) Interactions between the Mas-related receptors MrgD and MrgE alter signalling and trafficking of MrgD. Molecular Pharmacology, 69, pp. 479-491. (doi: 10.1124/mol.105.018788)

Milligan, G. (2006) G-protein-coupled receptor heterodimers: pharmacology, function and relevance to drug discovery. Drug Discovery Today, 11, pp. 541-549. (doi: 10.1016/j.drudis.2006.04.007)

Milligan, G. and Kostenis, E. (2006) Heterotrimeric G-proteins: a short history. British Journal of Pharmacology, 147, S46-S55.

Milligan, G. , Pediani, J., Canals, M. and Lopez-Gimenez, J. (2006) Oligomeric structure of the alpha(1b)-adrenoceptor: Comparisons with rhodopsin. Vision Research, 46, pp. 4434-4441. (doi: 10.1016/j.visres.2006.08.007)

Milligan, G. , Stoddart, L. and Brown, A. (2006) G protein-coupled receptors for free fatty acids. Cellular Signalling, 18, pp. 1360-1365. (doi: 10.1016/j.cellsig.2006.03.011)

Novotny, J., Durchankova, D., Ward, R., Carrillo, J., Svoboda, P. and Milligan, G. (2006) Functional interactions between the alpha(1b)-adrenoceptor and G alpha(11) are compromised by de-palmitoylation of the G protein but not of the receptor. Cellular Signalling, 18, pp. 1244-1251. (doi: 10.1016/j.cellsig.2005.10.004)

Snook, L., Milligan, G. , Kieffer, B. and Massotte, D. (2006) mu-delta opioid receptor functional interaction: Insight using receptor-G protein fusions. Journal of Pharmacology and Experimental Therapeutics, 318, pp. 683-690. (doi: 10.1124/jpet.106.101220)

2005

Milligan, G. and Bouvier, M. (2005) Methods to monitor the quaternary structure of G protein-coupled receptors. FEBS Journal, 272(12), pp. 2914-2925. (doi: 10.1111/j.1742-4658.2005.04731.x)

Barclay, E., OReilly, M. and Milligan, G. (2005) Activation of an alpha(2A)-adrenoceptor-G alpha(o1), fusion protein dynamically regulates the palmitoylation status of the G protein but not of the receptor. Biochemical Journal, 385, pp. 197-206.

Barnes, W., Reiter, E., Violin, J., Ren, X., Milligan, G. and Lefkowitz, R. (2005) beta-arrestin 1 and G(alpha q/11) coordinately activate RhoA and stress fiber formation following receptor stimulation. Journal of Biological Chemistry, 280, pp. 8041-8050. (doi: 10.1074/jbc.M412924200)

Holdsworth, G., Slocombe, P., Hutchinson, G. and Milligan, G. (2005) Analysis of endogenous S1P and LPA receptor expression in CHO-K1 cells. Gene, 350, pp. 59-63. (doi: 10.1016/j.gene.2005.01.016)

Hunton, D., Barnes, W., Kim, J., Ren, X., Violin, J., Reiter, E., Milligan, G. , Patel, D. and Lefkowitz, R. (2005) beta-arrestin 2-dependent angiotensin II type 1A receptor-mediated pathway of chemotaxis. Molecular Pharmacology, 67, pp. 1229-1236. (doi: 10.1124/mol.104.006270)

Kostenis, E., Martini, L., Ellis, J., Waldhoer, M., Heydorn, A., Rosenkilde, M., Norregaard, P., Jorgensen, R., Whistler, J. and Milligan, G. (2005) A highly conserved glycine within linker I and the extreme C terminus of G protein alpha subunits interact cooperatively in switching G protein-coupled receptor-to-effector specificity. Journal of Pharmacology and Experimental Therapeutics, 313, pp. 78-87. (doi: 10.1124/jpet.104.080424)

Kostenis, E. et al. (2005) (G)-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor. Circulation, 111, pp. 1806-1813. (doi: 10.1161/01.CIR.0000160867.23556.7D)

Kostenis, E., Waelbroeck, M. and Milligan, G. (2005) Techniques: Promiscuous G alpha proteins in basic research and drug discovery. Trends in Pharmacological Sciences, 26, pp. 595-602. (doi: 10.1016/j.tips.2005.09.007)

Milasta, S., Evans, N., Ormiston, L., Wilson, S., Lefkowitz, R. and Milligan, G. (2005) The sustainability of interactions between the orexin-1 receptor and beta-arrestin-2 is defined by a single C-terminal cluster of hydroxy amino acids and modulates the kinetics of ERK MAPK regulation. Biochemical Journal, 387, pp. 573-584.

Milligan, G. (2005) Opioid receptors and their interacting proteins. Neuromolecular Medicine, 7, pp. 51-59. (doi: 10.1385/NMM)

Milligan, G. , Wilson, S. and Lopez-Gimenez, J. (2005) The specificity and molecular basis of alpha(1)-adrenoceptor and CXCR chemokine receptor dimerization. Journal of Molecular Neuroscience, 26, pp. 161-167. (doi: 10.1385/JMN/26)

Murdoch, H., Feng, G., Bachner, D., Ormiston, L., White, J., Richter, D. and Milligan, G. (2005) Periplakin interferes with g protein activation by the melanin-concentrating hormone receptor-1 by binding to the proximal segment of the receptor C-terminal tail. Journal of Biological Chemistry, 280, pp. 8208-8220. (doi: 10.1074/jbc.M405215200)

Pascal, G. and Milligan, G. (2005) Functional complementation and the analysis of opioid receptor homodimerization. Molecular Pharmacology, 68, pp. 905-915. (doi: 10.1124/mol.105.013847)

Pediani, J., Colston, J., Caldwell, D., Milligan, G., Daly, C. and McGrath, J. (2005) beta-arrestin-dependent spontaneous alpha(1a)-adrenoceptor endocytosis causes intracellular transportation of alpha-blockers via recycling compartments. Molecular Pharmacology, 67, pp. 992-1004. (doi: 10.1124/mol.104.008417)

Rudajev, V., Novotny, J., Hejnova, L., Milligan, G. and Svoboda, P. (2005) Dominant portion of thyrotropin-releasing hormone receptor is excluded from lipid domains. Detergent-resistant and detergent-sensitive pools of TRH receptor and G(q)alpha/G(11)alpha protein. Journal of Biochemistry, 138, pp. 111-125. (doi: 10.1093/jb/mvi114)

Ward, R. and Milligan, G. (2005) A key serine for the GTPase-activating protein function of regulator of G protein signaling proteins is not a general target for 14-3-3 interactions. Molecular Pharmacology, 68, pp. 1821-1830. (doi: 10.1124/moi.105.015073) (PMID:16160139)

Wilson, S., Wilkinson, G. and Milligan, G. (2005) The CXCR1 and CXCR2 receptors form constitutive homo- and heterodimers selectively and with equal apparent affinities. Journal of Biological Chemistry, 280, pp. 28663-28674. (doi: 10.1074/jbc.M413475200)

2004

093114280 (2004) Materials and Methods Relating to G-Protein Coupled Receptor Oligomers. .

Milligan, G., Feng, G.J., Ward, R.J., Sartania, N. , Ramsay, D., McLean, A.J. and Carrillo, J.J. (2004) G protein-coupled receptor fusion proteins in drug discovery. Current Pharmaceutical Design, 10(17), pp. 1989-2001. (doi: 10.2174/1381612043384295) (PMID:15279540)

Bakker, R., Dees, G., Carrillo, J., Booth, R., Lopez-Gimenez, J., Milligan, G. , Strange, P. and Leurs, R. (2004) Domain swapping in the human histamine H-1 receptor. Journal of Pharmacology and Experimental Therapeutics, 311, pp. 131-138. (doi: 10.1124/jpet.104.067041)

Carrillo, J., Lopez-Gimenez, J. and Milligan, G. (2004) Multiple interactions between transmembrane helices generate the oligomeric alpha(1b)-adrenoceptor. Molecular Pharmacology, 66, pp. 1123-1137. (doi: 10.1124/mol.104.001586)

Heydorn, A., Ward, R., Jorgensen, R., Rosenkilde, M., Frimurer, T., Milligan, G. and Kostenis, E. (2004) Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interaction. Molecular Pharmacology, 66, pp. 250-259.

Holdsworth, G., Osborne, D.A., Thi Pham, T., Fells, J.I., Hutchinson, G., Milligan, G. and Parrill, A.L. (2004) A single amino acid determines preference between phospholipids and reveals length restriction for activation ofthe S1P₄ receptor. BMC Biochemistry, 5(12), (doi: 10.1186/1471-2091-5-12)

Klaasse, E., de Ligt, R., Roerink, S., Lorenzen, A., Milligan, G. , Leurs, R. and IJzerman, A. (2004) Allosteric modulation and constitutive activity of fusion proteins between the adenosine A(1) receptor and different (351)Cys-mutated G(i) alpha-subunits. European Journal of Pharmacology, 499, pp. 91-98. (doi: 10.1016/j.ejphar.2004.07.108)

Milligan, G. (2004) Applications of bioluminescence- and fluorescence resonance energy transfer to drug discovery at G protein-coupled receptors. European Journal of Pharmaceutical Sciences, 21, pp. 397-405. (doi: 10.1016/j.ejps.2003.11.010)

Milligan, G. (2004) G protein-coupled receptor dimerization: Function and ligand pharmacology. Molecular Pharmacology, 66, pp. 1-7. (doi: 10.1124/mol.104.000497)

Milligan, G. (2004) A single amino acid determines preference between phospholipids and reveals length restriction for activation ofthe S1P4 receptor. BMC Biochemistry, 5(12), pp. 1-12. (doi: 10.1186/1471-2091-5-12)

Milligan, G. , Lopez-Gimenez, J., Wilson, S. and Carrillo, J. (2004) Selectivity in the oligomerisation of G protein-coupled receptors. Seminars in Cell and Developmental Biology, 15, pp. 263-268. (doi: 10.1016/j.semcdb.2003.12.012)

Milligan, G. , Murdoch, H., Kellett, E., White, J. and Feng, G. (2004) Interactions between G-protein-coupled receptors and periplakin: a selective means to regulate G-protein activation. Biochemical Society Transactions, 32, pp. 878-880.

Milligan, G. , Pascal, G. and Carrillo, J. (2004) Monitoring receptor dimerisation. Medicinal Chemistry Research, 13, pp. 18-24.

Milligan, G. , Pediani, J., Fidock, M. and Lopez-Gimenez, J. (2004) Dimerization of alpha(1)-adrenoceptors. Biochemical Society Transactions, 32, pp. 847-850.

Moravcova, Z., Rudajev, V., Stohr, J., Novotny, J., Cerny, J., Parenti, M., Milligan, G. and Svoboda, P. (2004) Long-term agonist stimulation of IP prostanoid receptor depletes the cognate G(s)alpha protein in membrane domains but does not change the receptor level. Biochimica et Biophysica Acta: Molecular Cell Research, 1691, pp. 51-65. (doi: 10.1016/j.bbamcr.2003.12.004)

Ramsay, D., Carr, I., Pediani, J., Lopez-Gimenez, J., Thurlow, R., Fidock, M. and Milligan, G. (2004) High-affinity interactions between human alpha(1A)-adrenoceptor C-terminal splice variants produce homo- and heterodimers but do not generate the alpha(1L)-adrenoceptor. Molecular Pharmacology, 66, pp. 228-239.

Ward, R.J. and Milligan, G. (2004) Analysis of function of receptor-G-protein and receptor-RGS fusion proteins. Methods in Molecular Biology, 259, pp. 225-247. (PMID:15250496)

2003

60/472025 (2003) Materials and Methods Relating to G-Protein Coupled Receptor Oligomers. .

Adie, E., Francis, M., Davies, J., Smith, L., Marenghi, A., Hather, C., Hadingham, K., Michael, N., Milligan, G. and Gamel, S. (2003) CypHer 5: A generic approach for measuring the activation and trafficking of G protein-coupled receptors in live cells. Assay and Drug Development Technologies, 1, pp. 251-259.

Bahia, D. S., Sartania, N. , Ward, R. j., Cavalli, A., Jones, T. L.Z., Druey, K. M. and Milligan, G. (2003) Concerted stimulation and deactivation of pertussis toxin-sensitive G proteins by chimeric G protein-coupled receptor-regulator of G protein signaling 4 fusion proteins: analysis of the contribution of palmitoylated cysteine residues to the GAP activity o. Journal of Neurochemistry, 85(5), pp. 1289-1298. (doi: 10.1046/j.1471-4159.2003.01769.x) (PMID:12753087)

Benians, A., Leaney, J., Milligan, G. and Tinker, A. (2003) The dynamics of formation and action of the ternary complex revealed in living cells using a G-protein-gated K+ channel as a biosensor. Journal of Biological Chemistry, 278, pp. 10851-10858. (doi: 10.1074/jbc.M212299200)

Bertaso, F., Ward, R., Viard, P., Milligan, G. and Dolphin, A. (2003) Mechanism of action of G(q) to inhibit G beta gamma modulation of Ca(v)2.2 calcium channels: Probed by the use of receptor-G alpha tandems. Molecular Pharmacology, 63, pp. 832-843.

Bourova, L., Kostrnova, A., Hejnova, L., Moravcova, Z., Moon, H., Novotny, J., Milligan, G. and Svoboda, P. (2003) delta-Opioid receptors exhibit high efficiency when activating trimeric G proteins in membrane domains. Journal of Neurochemistry, 85, pp. 34-49. (doi: 10.1046/j.1471-4159.2003.01667.x)

Carrillo, J., Pediani, J. and Milligan, G. (2003) Dimers of class A G protein-coupled receptors function via agonist-mediated trans-activation of associated G proteins. Journal of Biological Chemistry, 278, pp. 42578-42587. (doi: 10.1074/jbc.M306165200)

Derrien, A., Zheng, B., Osterhout, J., Ma, Y., Milligan, G. , Farquhar, M. and Druey, K. (2003) Src-mediated RGS16 tyrosine phosphorylation promotes RGS16 stability. Journal of Biological Chemistry, 278, pp. 16107-16116. (doi: 10.1074/jbc.M210371200)

Feng, G., Kellett, E., Scorer, C., Wilde, J., White, J. and Milligan, G. (2003) Selective interactions between helix VIII of the human mu-opioid receptors and the C terminus of periplakin disrupt G protein activation. Journal of Biological Chemistry, 278, pp. 33400-33407. (doi: 10.1074/jbc.M305866200)

Hiol, A., Davey, P., Osterhout, J., Waheed, A., Fischer, E., Chen, C., Milligan, G., Druey, K. and Jones, T. (2003) Palmitoylation regulates regulators of G-protein signaling (RGS) 16 function - I. Mutation of amino-terminal cysteine residues on RGS16 prevents its targeting to lipid rafts and palmitoylation of an internal cysteine residue. Journal of Biological Chemistry, 278, pp. 19301-19308. (doi: 10.1074/jbc.M210123200) (PMID:12642593)

Milligan, G. (2003) Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective. Molecular Pharmacology, 64, pp. 1271-1276.

Milligan, G. (2003) High-content assays for ligand regulation of G-protein-coupled receptors. Drug Discovery Today, 8, pp. 579-585.

Milligan, G. (2003) Mechanism of action of Gq to inhibit Gbg modulation of Cav2.2 calcium channls probed by use of receptor-Ga tandems. Molecular Pharmacology, 63(4), pp. 832-843. (doi: 10.1124/mol.63.4.832)

Milligan, G. (2003) Principles: Extending the utility of [S-35]GTP gamma S binding assays. Trends in Pharmacological Sciences, 24, pp. 87-90.

Milligan, G. , Ramsay, D., Pascal, G. and Carrillo, J. (2003) GPCR dimerisation. Life Sciences, 74, pp. 181-188. (doi: 10.1016/j.lfs.2003.09.005)

Osterhout, J., Waheed, A., Hiol, A., Ward, R., Davey, P., Nini, L., Wang, J., Milligan, G., Jones, T. and Druey, K. (2003) Palmitoylation regulates regulator of G-protein signaling (RGS) 16 function - II. Palmitoylation of a cysteine residue in the RGS box is critical for RGS16 GTPase accelerating activity and regulation of G(i)-coupled signaling. Journal of Biological Chemistry, 278, pp. 19309-19316. (doi: 10.1074/jbc.M210124200) (PMID:12642592)

Zeng, F., McLean, A., Milligan, G. , Lerner, M., Chalmers, D. and Behan, D. (2003) Ligand specific up-regulation of a Renilla reniformis luciferase-tagged, structurally unstable muscarinic M-3 chimeric G protein-coupled receptor. Molecular Pharmacology, 64, pp. 1474-1484.

2002

Adamson, P., Wilbourn, B., Etienne-Manneville, S., Calder, V., Beraud, E., Milligan, G. , Couraud, P. and Greenwood, J. (2002) Lymphocyte trafficking through the blood-brain barrier is dependent on endothelial cell heterotrimeric G-protein signaling. FASEB Journal, 16,

Adie, E., Kalinka, S., Smith, L., Francis, M., Marenghi, A., Cooper, M., Briggs, M., Michael, N., Milligan, G. and Game, S. (2002) A pH-sensitive fluor, CypHer (TM) 5, used to monitor agonist-induced g protein-coupled receptor internalization in live cells. Biotechniques, 33, pp. 1152-1157.

Carrillo, J., Stevens, P. and Milligan, G. (2002) Measurement of agonist-dependent and -independent signal initiation of alpha(1b)-adrenoceptor mutants by direct analysis of guanine nucleotide exchange on the G protein G alpha(11). Journal of Pharmacology and Experimental Therapeutics, 302, pp. 1080-1088. (doi: 10.1124/jpet.102.035501)

Feng, G., Cavalli, A. and Milligan, G. (2002) Engineering a V-2 vasopressin receptor agonist- and regulator of G-protein-signaling-sensitive G protein. Analytical Biochemistry, 300, pp. 212-220. (doi: 10.1006/abio.2001.5448)

Liu, S., Carrillo, J., Pediani, J. and Milligan, G. (2002) Effective information transfer from the alpha(1b)-adrenoceptor to G alpha(11) requires both beta/gamma interactions and an aromatic group four amino acids from the C terminus of the G protein. Journal of Biological Chemistry, 277, pp. 25707-25714. (doi: 10.1074/jbc.M201015200)

Lyall, F., Lye, S., Teoh, T., Cousins, F., Milligan, G. and Robson, S. (2002) Expression of Gs alpha, connexin-43, connexin-26, and EP1, 3, and 4 receptors in myometrium of prelabor singleton versus multiple gestations and the effects of mechanical stretch and steroids on Gs alpha. Journal of the Society For Gynecologic Investigation, 9, pp. 299-307.

Massotte, D., Brillet, K., Kieffer, B. and Milligan, G. (2002) Agonists activate G(i1)alpha or G(i2)alpha fused to the human mu opioid receptor differently. Journal of Neurochemistry, 81, pp. 1372-1382.

McLean, A., Zeng, F., Behan, D., Chalmers, D. and Milligan, G. (2002) Generation and analysis of constitutively active and physically destabilized mutants of the human beta(1)-adrenoceptor. Molecular Pharmacology, 62, pp. 747-755.

Milligan, G. (2002) Construction and analysis of function of G protein-coupled receptor-G protein fusion proteins. G Protein Pathways, Pt A, Receptors, 343, pp. 260-273.

Milligan, G. (2002) Strategies to identify ligands for orphan G-protein-coupled receptors. Biochemical Society Transactions, 30, pp. 789-793.

Milligan, G. (2002) The use of receptor G-protein fusion proteins for the study of ligand activity. Receptors and Channels, 8, pp. 309-317. (doi: 10.1080/10606820290005281)

Milligan, G. , Stevens, P., Ramsay, D. and McLean, A. (2002) Ligand rescue of constitutively active mutant receptors. Neurosignals, 11, pp. 29-33.

Ramsay, D., Kellett, E., McVey, M. , Rees, S. and Milligan, G. (2002) Homo- and hetero-oligomeric interactions between G-protein-coupled receptors in living cells monitored by two variants of bioluminescence resonance energy transfer (BRET): hetero-oligomers between receptor subtypes form more efficiently than between less. Biochemical Journal, 365, pp. 429-440. (doi: 10.1042/BJ20020251)

Ward, R. and Milligan, G. (2002) Reciprocal mutations of highly conserved residues in transmembrane helices 2 and 7 of the alpha(2A)-adrenoceptor restore agonist activation of G(i1 alpha). Cellular Signalling, 14, pp. 139-144.

Welsby, P., Carr, I., Wilkinson, G. and Milligan, G. (2002) Regulation of the avidity of ternary complexes containing the human 5-HT1A receptor by mutation of a receptor contact site on the interacting G protein alpha subunit. British Journal of Pharmacology, 137, pp. 345-352. (doi: 10.1038/sj.bjp.0704880)

Welsby, P., Kellett, E., Wilkinson, G. and Milligan, G. (2002) Enhanced detection of receptor constitutive activity in the presence of regulators of G protein signaling: Applications to the detection and analysis of inverse agonists and low-efficacy partial agonists. Molecular Pharmacology, 61, pp. 1211-1221.

2001

Milligan, G. and White, J. H. (2001) Protein-protein interactions at G-protein-coupled receptors. Trends in Pharmacological Sciences, 22(10), pp. 513-518. (doi: 10.1016/S0165-6147(00)01801-0)

Evans, N., Groarke, D., Warrack, J., Greenwood, C., Dodgson, K., Milligan, G. and Wilson, S. (2001) Visualizing differences in ligand-induced beta-arrestin-GFP interactions and trafficking between three recently characterized G protein-coupled receptors. Journal of Neurochemistry, 77, pp. 476-485.

Fernandez-Fernandez, J., Abogadie, F., Milligan, G. , Delmas, P. and Brown, D. (2001) Multiple pertussis toxin-sensitive G-proteins can couple receptors to GIRK channels in rat sympathetic neurons when expressed heterologously, but only native G(i)-proteins do so in situ. European Journal of Neuroscience, 14, pp. 283-292.

Groarke, D., Drmota, T., Bahia, D., Evans, N., Wilson, S. and Milligan, G. (2001) Analysis of the C-terminal tail of the rat thyrotropin-releasing hormone receptor-1 in interactions and cointernalization with beta-arrestin 1-green fluorescent protein. Molecular Pharmacology, 59, pp. 375-385.

Hoffmann, M., Ward, R., Cavalli, A., Carr, I. and Milligan, G. (2001) Differential capacities of the RGS1, RGS16 and RGS-GAIP regulators of G protein signaling to enhance alpha(2A)-adrenoreceptor agonist-stimulated GTPase activity of G(o1)alpha. Journal of Neurochemistry, 78, pp. 797-806.

McVey, M., Ramsay, D., Kellett, E., Rees, S., Wilson, S., Pope, A. and Milligan, G. (2001) Monitoring receptor oligomerization using time-resolved fluorescence resonance energy transfer and bioluminescence resonance energy transfer - The human delta-opioid receptor displays constitutive oligomerization at the cell surface, which is not regulate. Journal of Biological Chemistry, 276, pp. 14092-14099.

Millan, M. et al. (2001) Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: Cellular and functional characterization. Journal of Pharmacology and Experimental Therapeutics, 297, pp. 876-887.

Milligan, G. (2001) The human d opioid receptor activates Gi1a more efficiently than Go1a. Journal of Neurochemistry, 76(6), pp. 1805-1813. (doi: 10.1046/j.1471-4159.2001.00196.x)

Milligan, G. (2001) Oligomerisation of G-protein-coupled receptors. Journal of Cell Science, 114, pp. 1265-1271.

Milligan, G. , Kellett, E., Dacquet, C., Dubreuil, V., Jacoby, E., Millan, M., Lavielle, G. and Spedding, M. (2001) S 14506: novel receptor coupling at 5-HT1A receptors. Neuropharmacology, 40, pp. 334-344.

Moon, H., Bahia, D., Cavalli, A., Hoffmann, M. and Milligan, G. (2001) Control of the efficiency of agonist-induced information transfer and stability of the ternary complex containing the delta opioid receptor and the alpha subunit of G(i1) by mutation of a receptor/G protein contact interface. Neuropharmacology, 41, pp. 321-330.

Moon, H., Cavalli, A., Bahia, D., Hoffmann, M., Massotte, D. and Milligan, G. (2001) The human delta opioid receptor activates G(i1)alpha more efficiently than G(o1)alpha. Journal of Neurochemistry, 76, pp. 1805-1813.

Ramsay, D., Bevan, N., Rees, S. and Milligan, G. (2001) Detection of receptor ligands by monitoring selective stabilization of a Renilla luciferase-tagged, constitutively active mutant, G-protein-coupled receptor. British Journal of Pharmacology, 133, pp. 315-323.

Stevens, P., Pediani, J., Carrillo, J. and Milligan, G. (2001) Coordinated agonist regulation of receptor and G protein palmitoylation and functional rescue of palmitoylation-deficient mutants of the G protein G(11)alpha following fusion to the alpha(1b)-adrenoreceptor - Palmitoylation of G(11 alpha) is not required. Journal of Biological Chemistry, 276, pp. 35883-35890.

1998

Daly, C.J. , Milligan, C.M., Milligan, G. , Mackenzie, J.F. and McGrath, J.C. (1998) Cellular localization and pharmacological characterization of functioning alpha-1 adrenoceptors by fluorescent ligand binding and image analysis reveals identical binding properties of clustered and diffuse populations of receptors. Journal of Pharmacology and Experimental Therapeutics, 286(2), pp. 984-990.

1993

Ross, B. M., McLaughlin, M. , Roberts, M., Milligan, G. , McCulloch, J. and Knowler, J. T. (1993) Alterations in the activity of adenylate cyclase and high affinity GTPase in Alzheimer's disease. Brain Research, 622(1-2), pp. 35-42. (doi: 10.1016/0006-8993(93)90798-R) (PMID:8242380)

1991

McLaughlin, M. , Ross, B. M., Milligan, G. , McCulloch, J. and Knowler, J. T. (1991) Robustness of G proteins in Alzheimer's disease: an immunoblot study. Journal of Neurochemistry, 57(1), pp. 9-14. (doi: 10.1111/j.1471-4159.1991.tb02092.x) (PMID:1904911)

1987

Pyne, N.J., Anderson, N., Lavan, B.E., Milligan, G. , Nimmo, H.G. and Houslay, M.D. (1987) Specific antibodies and the selective inhibitor ICI 118233 demonstrate that the hormonally stimulated 'dense-vesicle' and peripheral-plasma-membrane cyclic AMP phosphodiesterases display distinct tissue distributions in the rat. Biochemical Journal, 248(3), pp. 897-901. (doi: 10.1042/bj2480897) (PMID:2829845) (PMCID:PMC1148634)

Articles

Quon, T., Lin, L.-C., Ganguly, A. , Hudson, B. D. , Tobin, A. B. and Milligan, G. (2024) Biased constitutive signalling of the G protein-coupled receptor GPR35 suppresses gut barrier permeability. Journal of Biological Chemistry, (Accepted for Publication)

Brettell, S. B. et al. (2024) Targeting PfCLK3 with covalent inhibitors: a novel strategy for malaria treatment. Journal of Medicinal Chemistry, (doi: 10.1021/acs.jmedchem.4c01300) (PMID:39441986) (Early Online Publication)

Marsango, S. and Milligan, G. (2024) Regulation of the pro-inflammatory G protein-coupled receptor GPR84. British Journal of Pharmacology, 181(10), pp. 1500-1508. (doi: 10.1111/bph.16098) (PMID:37085331)

Milligan, G. (2024) Editorial for GPR84 Pharmacology. British Journal of Pharmacology, 181(10), pp. 1497-1499. (doi: 10.1111/bph.16340)

Tikhonova, I., Zhang, X., Guseinov, A.-A., Jenkins, L. , Li, K., Milligan, G. and Zhang, C. (2024) Structural basis for the ligand recognition and signaling of free fatty acid receptors. Science Advances, 10(2), eadj2384. (doi: 10.1126/sciadv.adj2384) (PMID:38198545)

Barki, N. et al. (2023) Phosphorylation bar-coding of free fatty acid receptor 2 is generated in a tissue-specific manner. eLife, 12, RP91861. (doi: 10.7554/eLife.91861) (PMID:38085667) (PMCID:PMC10715726)

Kalita, M. et al. (2023) PET imaging of innate immune activation using 11C radiotracers targeting GPR84. JACS Au, 3(12), pp. 3297-3310. (doi: 10.1021/jacsau.3c00435) (PMID:38155640) (PMCID:PMC10751761)

Ganguly, A. et al. (2023) G protein-receptor kinases 5/6 are the key regulators of G protein-coupled receptor 35-arrestin interactions. Journal of Biological Chemistry, 299(10), 105218. (doi: 10.1016/j.jbc.2023.105218) (PMID:37660910) (PMCID:PMC10520886)

Zhang, X. et al. (2023) Pro-phagocytic function and structural basis of GPR84 signaling. Nature Communications, 14, 5706. (doi: 10.1038/s41467-023-41201-0) (PMID:37709767) (PMCID:PMC10502086)

Valentini, A., Schultz-Knudsen, K., Højgaard Hansen, A., Tsakoumagkou, A., Jenkins, L. , Christensen, H. B., Manandhar, A., Milligan, G. , Ulven, T. and Rexen Ulven, E. (2023) Discovery of potent tetrazole free fatty acid receptor 2 antagonists. Journal of Medicinal Chemistry, 66(9), pp. 6105-6121. (doi: 10.1021/acs.jmedchem.2c01935) (PMID:37129317)

Milligan, G. (2023) GPR35: from enigma to therapeutic target. Trends in Pharmacological Sciences, 44(5), pp. 263-273. (doi: 10.1016/j.tips.2023.03.001) (PMID:37002007)

Meda Venkata, S. P., Li, H., Xu, L., Koh, J. Y., Nguyen, H., Minjares, M., Li, C., Kowluru, A., Milligan, G. and Wang, J.-M. (2023) Inhibition of GPR39 restores defects in endothelial cell–mediated neovascularization under the duress of chronic hyperglycemia: evidence for regulatory roles of the sonic hedgehog signaling axis. Proceedings of the National Academy of Sciences of the United States of America, 120(1), e2208541120. (doi: 10.1073/pnas.2208541120) (PMID:36574661) (PMCID:PMC9910611)

Alharbi, A. G., Tobin, A. B. and Milligan, G. (2022) How arrestins and GRKs regulate the function of long chain fatty acid receptors. International Journal of Molecular Sciences, 23(20), 12237. (doi: 10.3390/ijms232012237) (PMID:36293091) (PMCID:PMC9602559)

Mahindra, A. et al. (2022) Investigating the structure–activity relationship of 1,2,4-triazine G-protein-coupled receptor 84 (GPR84) antagonists. Journal of Medicinal Chemistry, 65(16), pp. 11270-11290. (doi: 10.1021/acs.jmedchem.2c00804) (PMID:35948061) (PMCID:PMC9421653)

Marsango, S., Barki, N., Jenkins, L. , Tobin, A. B. and Milligan, G. (2022) Therapeutic validation of an orphan G protein-coupled receptor: the case of GPR84. British Journal of Pharmacology, 179(14), pp. 3529-3541. (doi: 10.1111/bph.15248) (PMID:32869860) (PMCID:PMC9361006)

Marsango, S. et al. (2022) The M1 muscarinic receptor is present in situ as a ligand-regulated mixture of monomers and oligomeric complexes. Proceedings of the National Academy of Sciences of the United States of America, 119(24), e220110311. (doi: 10.1073/pnas.2201103119) (PMID:35671422) (PMCID:PMC9214538)

Caspar, B., Cocchiara, P., Melet, A., Van Emelen, K., Van der Aa, A., Milligan, G. and Herbeuval, J.-P. (2022) CXCR4 as a novel target in immunology: moving away from typical antagonists. Future Drug Discovery, 4(2), FDD77. (doi: 10.4155/fdd-2022-0007) (PMID:35875591) (PMCID:PMC9298491)

Marsango, S. et al. (2022) Selective phosphorylation of threonine residues defines GPR84-arrestin interactions of biased ligands. Journal of Biological Chemistry, 298(5), 101932. (doi: 10.1016/j.jbc.2022.101932) (PMID:35427647) (PMCID:PMC9118924)

Barki, N. et al. (2022) Chemogenetics defines the roles of short chain fatty acid receptors within the gut-brain axis. eLife, 11, e73777. (doi: 10.7554/eLife.73777) (PMID:35229717) (PMCID:PMC8887895)

Divorty, N., Jenkins, L. , Ganguly, A. , Butcher, A. J., Hudson, B. D. , Schulz, S., Tobin, A. B. , Nicklin, S. A. and Milligan, G. (2022) Agonist-induced phosphorylation of orthologues of the orphan receptor GPR35 functions as an activation sensor. Journal of Biological Chemistry, 298(3), 101655. (doi: 10.1016/j.jbc.2022.101655) (PMID:35101446) (PMCID:PMC8892012)

Scarpa, M. et al. (2021) Biased M1 muscarinic receptor mutant mice show accelerated progression of prion neurodegenerative disease. Proceedings of the National Academy of Sciences of the United States of America, 118(50), e2107389118. (doi: 10.1073/pnas.2107389118) (PMID:34893539) (PMCID:PMC8685681)

Lin, L.-C., Quon, T., Engberg, S., Mackenzie, A. E., Tobin, A. B. and Milligan, G. (2021) G protein-coupled receptor GPR35 suppresses lipid accumulation in hepatocytes. ACS Pharmacology and Translational Science, 4(6), pp. 1835-1848. (doi: 10.1021/acsptsci.1c00224) (PMID:34927014)

Milligan, G. et al. (2021) Discovery and characterization of novel antagonists of the proinflammatory orphan receptor GPR84. ACS Pharmacology and Translational Science, 4(5), pp. 1598-1613. (doi: 10.1021/acsptsci.1c00151) (PMID:34661077) (PMCID:PMC8506611)

Boleij, A. et al. (2021) G-protein coupled receptor 35 (GPR35) regulates the colonic epithelial cell response to enterotoxigenic Bacteroides fragilis. Communications Biology, 4, 585. (doi: 10.1038/s42003-021-02014-3) (PMID:33990686) (PMCID:PMC8121840)

Milligan, G. , Barki, N. and Tobin, A. (2021) Chemogenetic approaches to explore the functions of Free Fatty Acid Receptor 2. Trends in Pharmacological Sciences, 42(3), pp. 191-202. (doi: 10.1016/j.tips.2020.12.003) (PMID:33495026)

Bolognini, D., Dedeo, D. and Milligan, G. (2021) Metabolic and inflammatory functions of short-chain fatty acid receptors. Current Opinion in Endocrine and Metabolic Research, 16, pp. 1-9. (doi: 10.1016/j.coemr.2020.06.005) (PMID:32835130) (PMCID:PMC7332907)

Ward, R. J., Pediani, J. D. , Marsango, S., Jolly, R., Stoneman, M. R., Biener, G., Handel, T. M., Raicu, V. and Milligan, G. (2021) Chemokine receptor CXCR4 oligomerization is disrupted selectively by the antagonist ligand IT1t. Journal of Biological Chemistry, 296, 100139. (doi: 10.1074/jbc.RA120.016612) (PMID:33268380)

Marti-Solano, M. et al. (2020) Combinatorial expression of GPCR isoforms affects signalling and drug responses. Nature, 587, pp. 650-656. (doi: 10.1038/s41586-020-2888-2) (PMID:33149304)

Labéguère, F. et al. (2020) Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a unique GPR84 negative allosteric modulator undergoing evaluation in a phase II clinical trial. Journal of Medicinal Chemistry, 63(22), pp. 13526-13545. (doi: 10.1021/acs.jmedchem.0c00272) (PMID:32902984)

Prihandoko, R. et al. (2020) Pathophysiological regulation of lung function by the free fatty acid receptor FFA4. Science Translational Medicine, 12(557), eaaw9009. (doi: 10.1126/scitranslmed.aaw9009) (PMID:32817367)

Quon, T., Lin, L.-C., Ganguly, A. , Tobin, A. B. and Milligan, G. (2020) Therapeutic opportunities and challenges in targeting the orphan G protein-coupled receptor GPR35. ACS Pharmacology and Translational Science, 3(5), pp. 801-812. (doi: 10.1021/acsptsci.0c00079) (PMID:33073184)

Rexen Ulven, E. et al. (2020) Structure-activity relationship studies of tetrahydroquinolone free fatty acid receptor 3 modulators. Journal of Medicinal Chemistry, 63(7), pp. 3577-3595. (doi: 10.1021/acs.jmedchem.9b02036) (PMID:32141297) (PMCID:PMC7307922)

Sencio, V. et al. (2020) Gut dysbiosis during influenza contributes to pulmonary pneumococcal superinfection through altered short-chain fatty acid production. Cell Reports, 30(9), 2934-2947.e6. (doi: 10.1016/j.celrep.2020.02.013) (PMID:32130898)

Heuninck, J. et al. (2019) Context-dependent signaling of CXC chemokine receptor 4 and atypical chemokine receptor 3. Molecular Pharmacology, 96(6), pp. 778-793. (doi: 10.1124/mol.118.115477) (PMID:31092552)

Stoneman, M. R., Biener, G., Ward, R. J., Pediani, J. D. , Badu, D., Eis, A., Popa, I., Milligan, G. and Raicu, V. (2019) A general method to quantify ligand-driven oligomerization from fluorescence-based images. Nature Methods, 16(6), pp. 493-496. (doi: 10.1038/s41592-019-0408-9) (PMID:31110281)

Bolognini, D. et al. (2019) Chemogenetics defines receptor-mediated functions of short chain free fatty acids. Nature Chemical Biology, 15(5), pp. 489-498. (doi: 10.1038/s41589-019-0270-1) (PMID:30992568)

Mackenzie, A. E., Quon, T., Lin, L.-C., Hauser, A. S., Jenkins, L. , Inoue, A., Tobin, A. B. , Gloriam, D. E., Hudson, B. D. and Milligan, G. (2019) Receptor selectivity between the G proteins Gα12 and Gα13 is defined by a single leucine-to-isoleucine variation. FASEB Journal, 33(4), pp. 5005-5017. (doi: 10.1096/fj.201801956R) (PMID:30601679) (PMCID:PMC6436656)

Milligan, G. , Ward, R. J. and Marsango, S. (2019) GPCR homo-oligomerization. Current Opinion in Cell Biology, 57, pp. 40-47. (doi: 10.1016/j.ceb.2018.10.007) (PMID:30453145) (PMCID:PMC7083226)

Mancini, S., Mahmud, Z. A., Jenkins, L. , Bolognini, D., Newman, R., Barnes, M., Edye, M. E., McMahon, S. B., Tobin, A. B. and Milligan, G. (2019) On-target and off-target effects of novel orthosteric and allosteric activators of GPR84. Scientific Reports, 9, 1861. (doi: 10.1038/s41598-019-38539-1) (PMID:30755705) (PMCID:PMC6372602)

Müskens, F. M., Ward, R. J., Herkt, D., van de Langemheen, H., Tobin, A. B. , Liskamp, R. M.J. and Milligan, G. (2019) Design, synthesis and evaluation of a diazirine photoaffinity probe for ligand-based receptor capture targeting G protein-coupled receptors. Molecular Pharmacology, 95(2), pp. 196-209. (doi: 10.1124/mol.118.114249) (PMID:30514721) (PMCID:PMC6324650)

Kennedy, A. J., Ballante, F., Johansson, J. R., Milligan, G. , Sunström, L., Nordqvist, A. and Carlsson, J. (2018) Structural characterization of agonist binding to protease-activated receptor 2 through mutagenesis and computational modeling. ACS Pharmacology and Translational Science, 1(2), pp. 119-133. (doi: 10.1021/acsptsci.8b00019)

Hansen, A. H., Sergeev, E. , Bolognini, D., Sprenger, R. R., Ekberg, J. H., Ejsing, C. S., McKenzie, C. J., Rexen Ulven, E., Milligan, G. and Ulven, T. (2018) Discovery of a potent thiazolidine free fatty acid receptor 2 agonist with favorable pharmacokinetic properties. Journal of Medicinal Chemistry, 61(21), pp. 9534-9550. (doi: 10.1021/acs.jmedchem.8b00855) (PMID:30247908)

Drew, J. E. et al. (2018) Dietary fibers inhibit obesity in mice, but host responses in the cecum and liver appear unrelated to fiber-specific changes in cecal taxonomic composition. Scientific Reports, 8, 15566. (doi: 10.1038/s41598-018-34081-8) (PMID:30349136) (PMCID:PMC6197265)

Divorty, N., Milligan, G. , Graham, D. and Nicklin, S. A. (2018) The orphan receptor GPR35 contributes to angiotensin II–induced hypertension and cardiac dysfunction in mice. American Journal of Hypertension, 31(9), pp. 1049-1058. (doi: 10.1093/ajh/hpy073) (PMID:29860395) (PMCID:PMC6077831)

Marsango, S., Ward, R. J., Alvarez-Curto, E. and Milligan, G. (2018) Muscarinic receptor oligomerization. Neuropharmacology, 136(Part C), pp. 401-410. (doi: 10.1016/j.neuropharm.2017.11.023) (PMID:29146505) (PMCID:PMC6078712)

Binti Mohd Amir, N. A.S., Mackenzie, A. E., Jenkins, L. , Boustani, K., Hillier, M. C., Tsuchiya, T., Milligan, G. and Pease, J. E. (2018) Evidence for the existence of a CXCL17 receptor distinct from GPR35. Journal of Immunology, 201(2), pp. 714-724. (doi: 10.4049/jimmunol.1700884) (PMID:29875152) (PMCID:PMC6036231)

Milligan, G. (2018) G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35. British Journal of Pharmacology, 175(13), pp. 2543-2553. (doi: 10.1111/bph.14042) (PMID:28940377) (PMCID:PMC6003633)

Milligan, G. and Inoue, A. (2018) Genome editing provides new insights into receptor-controlled signalling pathways. Trends in Pharmacological Sciences, 39(5), pp. 481-493. (doi: 10.1016/j.tips.2018.02.005) (PMID:29548548)

Pediani, J. D. , Ward, R. J., Marsango, S. and Milligan, G. (2018) Spatial intensity distribution analysis: studies of G Protein-coupled receptor oligomerization. Trends in Pharmacological Sciences, 39(2), pp. 175-186. (doi: 10.1016/j.tips.2017.09.001) (PMID:29032835) (PMCID:PMC5783713)

Reichardt, N. et al. (2018) Specific substrate-driven changes in human faecal microbiota composition contrast with functional redundancy in short-chain fatty acid production. ISME Journal, 12, pp. 610-622. (doi: 10.1038/ismej.2017.196) (PMID:29192904)

Mahmud, Z. A., Jenkins, L. , Ulven, T., Labéguère, F., Gosmini, R., De Vos, S., Hudson, B. D. , Tikhonova, I. G. and Milligan, G. (2017) Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84. Scientific Reports, 7, 17953. (doi: 10.1038/s41598-017-18159-3) (PMID:29263400) (PMCID:PMC5738391)

Viskaitis, P. et al. (2017) Modulation of SF1 neuron activity coordinately regulates both feeding behaviour and associated emotional states. Cell Reports, 21(12), pp. 3559-3572. (doi: 10.1016/j.celrep.2017.11.089) (PMID:29262334) (PMCID:PMC5746599)

Sergeev, E. , Hansen, A. H., Bolognini, D., Kawakami, K., Kishi, T., Aoki, J., Ulven, T., Inoue, A., Hudson, B. D. and Milligan, G. (2017) A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias. Scientific Reports, 7, 13741. (doi: 10.1038/s41598-017-14096-3) (PMID:29061999) (PMCID:PMC5653858)

Milligan, G. , Alvarez-Curto, E. , Hudson, B. D. , Prihandoko, R. and Tobin, A. B. (2017) FFA4/GPR120: pharmacology and therapeutic opportunities. Trends in Pharmacological Sciences, 38(9), pp. 809-821. (doi: 10.1016/j.tips.2017.06.006) (PMID:28734639) (PMCID:PMC5582618)

Prokop, S., Perry, N. A., Vishnivetskiy, S. A., Toth, A. D., Inoue, A., Milligan, G. , Iverson, T. M., Hunyady, L. and Gurevich, V. V. (2017) Differential manipulation of arrestin-3 binding to basal and agonist-activated G protein-coupled receptors. Cellular Signalling, 36, pp. 98-107. (doi: 10.1016/j.cellsig.2017.04.021) (PMID:28461104)

Lopez-Gimenez, J., Alvarez-Curto, E. and Milligan, G. (2017) M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes. Cellular Signalling, 35, pp. 208-222. (doi: 10.1016/j.cellsig.2017.04.006) (PMID:28411124)

Kaspersen, M. H., Jenkins, L. , Dunlop, J. , Milligan, G. and Ulven, T. (2017) Succinct synthesis of saturated hydroxy fatty acids and in vitro evaluation of all hydroxylauric acids on FFA1, FFA4 and GPR84. MedChemComm, 8(6), pp. 1360-1365. (doi: 10.1039/c7md00130d)

Ward, R. J., Pediani, J. D. , Harikumar, K. G., Miller, L. J. and Milligan, G. (2017) Spatial intensity distribution analysis quantifies the extent and regulation of homodimerization of the secretin receptor. Biochemical Journal, 474(11), pp. 1879-1895. (doi: 10.1042/BCJ20170184) (PMID:28424368) (PMCID:PMC5442643)

Watterson, K. R. et al. (2017) Probe-dependent negative allosteric modulators of the long-chain free fatty acid receptor FFA4. Molecular Pharmacology, 91(6), pp. 630-641. (doi: 10.1124/mol.116.107821) (PMID:28385906) (PMCID:PMC5438128)

Marsango, S., Caltabiano, G., Jiménez-Rosés, M., Millan, M. J., Pediani, J. D. , Ward, R. J. and Milligan, G. (2017) A molecular basis for selective antagonist destabilization of dopamine D3 receptor quaternary organization. Scientific Reports, 7, 2134. (doi: 10.1038/s41598-017-02249-3) (PMID:28522847) (PMCID:PMC5437050)

Houthuijzen, J. M. et al. (2017) Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance. FASEB Journal, 31(5), pp. 2195-2209. (doi: 10.1096/fj.201601248R) (PMID:28183801) (PMCID:PMC5388545)

Mackenzie, A. E. and Milligan, G. (2017) The emerging pharmacology and function of GPR35 in the nervous system. Neuropharmacology, 113(part B), pp. 661-671. (doi: 10.1016/j.neuropharm.2015.07.035) (PMID:26232640)

Hansen, A. H., Sergeev, E. , Pandey, S. K., Hudson, B. D. , Christiansen, E., Milligan, G. and Ulven, T. (2017) Development and characterization of a fluorescent tracer for the free fatty acid receptor 2 (FFA2/GPR43). Journal of Medicinal Chemistry, 60(13), pp. 5638-5645. (doi: 10.1021/acs.jmedchem.7b00338) (PMID:28570808)

Milligan, G. , Shimpukade, B., Ulven, T. and Hudson, B. D. (2017) Complex pharmacology of free fatty acid receptors. Chemical Reviews, 117(1), pp. 67-110. (doi: 10.1021/acs.chemrev.6b00056) (PMID:27299848)

Alvarez-Curto, E. , Inoue, A., Jenkins, L. , Raihan, S. Z., Prihandoko, R., Tobin, A. B. and Milligan, G. (2016) Targeted elimination of G proteins and arrestins defines their specific contributions to both intensity and duration of G protein-coupled receptor signalling. Journal of Biological Chemistry, 291(53), pp. 27147-27159. (doi: 10.1074/jbc.M116.754887) (PMID:27852822) (PMCID:PMC5207144)

Azevedo, C. M. G. et al. (2016) Non-acidic free fatty acid receptor 4 agonists with antidiabetic activity. Journal of Medicinal Chemistry, 59(19), pp. 8868-8878. (doi: 10.1021/acs.jmedchem.6b00685)

Bolognini, D. et al. (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. Journal of Biological Chemistry, 291, pp. 18915-18931. (doi: 10.1074/jbc.M116.736157) (PMID:27385588) (PMCID:PMC5009265)

Alvarez-Curto, E. and Milligan, G. (2016) Metabolism meets immunity: the role of free fatty acid receptors in the immune system. Biochemical Pharmacology, 114, pp. 3-13. (doi: 10.1016/j.bcp.2016.03.017) (PMID:27002183)

Pediani, J. D. , Ward, R. J., Godin, A. G., Marsango, S. and Milligan, G. (2016) Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs. Journal of Biological Chemistry, 291, pp. 13132-13146. (doi: 10.1074/jbc.M115.712562) (PMID:27080256) (PMCID:PMC4933229)

Nuber, S., Zabel, U., Lorenz, K., Nuber, A., Milligan, G. , Tobin, A. B. , Lohse, M. J. and Hoffmann, C. (2016) β-Arrestin biosensors reveal a rapid, receptor-dependent activation/deactivation cycle. Nature, 531, pp. 661-664. (doi: 10.1038/nature17198) (PMID:27007855)

Hansen, S. V.F. et al. (2016) Discovery of a potent free fatty acid 1 receptor agonist with low lipophilicity, low polar surface area and robust in vivo efficacy. Journal of Medicinal Chemistry, 59, pp. 2841-2846. (doi: 10.1021/acs.jmedchem.5b01962)

Grundmann, M., Tikhonova, I. G., Hudson, B. D. , Smith, N. J., Mohr, K., Ulven, T., Milligan, G. , Kenakin, T. and Kostenis, E. (2016) A molecular mechanism for sequential activation of a G Protein-coupled receptor. Cell Chemical Biology, 23(3), pp. 392-403. (doi: 10.1016/j.chembiol.2016.02.014) (PMID:26991104)

Bolognini, D., Tobin, A. B. , Milligan, G. and Moss, C. E. (2016) The pharmacology and function of receptors for short-chain fatty acids. Molecular Pharmacology, 89(3), pp. 388-398. (doi: 10.1124/mol.115.102301) (PMID:26719580)

Moreno, J. L. et al. (2016) Allosteric signaling through an mGlu2 and 5-HT2A heteromeric receptor complex and its potential contribution to schizophrenia. Science Signaling, 9(410), ra5. (doi: 10.1126/scisignal.aab0467) (PMID:26758213) (PMCID:PMC4819166)

Sergeev, E. , Hansen, A. H., Pandey, S. K., MacKenzie, A. E., Hudson, B. D. , Ulven, T. and Milligan, G. (2016) Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands. Journal of Biological Chemistry, 291, pp. 303-317. (doi: 10.1074/jbc.M115.687939) (PMID:26518871) (PMCID:PMC4697166)

Christiansen, E., Hudson, B. D. , Hansen, A. H., Milligan, G. and Ulven, T. (2016) Development and characterization of a potent free fatty acid receptor 1 (FFA1) fluorescent tracer. Journal of Medicinal Chemistry, 59(10), pp. 4849-4858. (doi: 10.1021/acs.jmedchem.6b00202) (PMID:27074625)

McCallum, J. E., Mackenzie, A. E., Divorty, N., Clarke, C., Delles, C. , Milligan, G. and Nicklin, S. A. (2016) G protein-coupled receptor 35 mediates human saphenous vein vascular smooth muscle cell migration and endothelial cell proliferation. Journal of Vascular Research, 52(6), pp. 383-395. (doi: 10.1159/000444754) (PMID:27064272) (PMCID:PMC4959467)

Prihandoko, R., Alvarez-Curto, E. , Hudson, B. D. , Butcher, A. J., Ulven, T., Miller, A. M., Tobin, A. B. and Milligan, G. (2016) Distinct phosphorylation clusters determines the signalling outcome of the free fatty acid receptor FFA4/GPR120. Molecular Pharmacology, 89(5), pp. 505-520. (doi: 10.1124/mol.115.101949) (PMID:26873857)

Schrage, R. et al. (2015) The experimental power of FR900359 to study Gq-regulated biological processes. Nature Communications, 6, p. 10156. (doi: 10.1038/ncomms10156) (PMID:26658454) (PMCID:PMC4682109)

Brown, J.H., Catterall, W.A., Conn, P.J., Cull-Candy, S.G., Dingledine, R., Harden, T.K., Insel, P.A., Milligan, G. and Traynelis, S.F. (2015) The first 50 years of molecular pharmacology. Molecular Pharmacology, 88(1), pp. 139-140. (doi: 10.1124/mol.115.099564) (PMID:25943115)

Mckinney, C.A., Kennedy, S. , Baillie, G.S. , Milligan, G. and Nicklin, S.A. (2015) Angiotensin-(1-7) and angiotensin-(1-9) inhibit vascular smooth muscle cell growth and migration in vitro and vascular remodelling in vivo. Atherosclerosis, 241(1), e44. (doi: 10.1016/j.atherosclerosis.2015.04.158)

Milligan, G. , Alvarez-Curto, E. , Watterson, K.R., Ulven, T. and Hudson, B.D. (2015) Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4. British Journal of Pharmacology, 172(13), pp. 3254-3265. (doi: 10.1111/bph.12879) (PMID:25131623)

Marsango, S., Caltabiano, G., Pou, C., Varela Liste, M. J. and Milligan, G. (2015) Analysis of human dopamine D3 receptor quaternary structure. Journal of Biological Chemistry, 290, pp. 15146-15162. (doi: 10.1074/jbc.M114.630681) (PMID:25931118) (PMCID:PMC4463457)

Milligan, G. , Liste, M. J. V., Caltabiano, G. C., Alvarez-Curto, E. and Marsango, S. (2015) Defining the organizational structure of dopamine and muscarninic acetylcholine receptors. SpringerPlus, 4(Sup 1), L7. (doi: 10.1186/2193-1801-4-s1-l7) (PMID:27386224) (PMCID:PMC4796694)

Aslanoglou, D., Alvarez-Curto, E. , Marsango, S. and Milligan, G. (2015) Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers. Journal of Biological Chemistry, 290(23), pp. 14785-14796. (doi: 10.1074/jbc.M115.649079) (PMID:25918156) (PMCID:PMC4505543)

Christiansen, E. et al. (2015) Activity of dietary fatty acids on FFA1 and FFA4 and characterisation of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases. British Journal of Nutrition, 113(11), pp. 1677-1688. (doi: 10.1017/S000711451500118X) (PMID:25916176)

Liste, M. J., Caltabiano, G., Ward, R. J., Alvarez-Curto, E. , Marsango, S. and Milligan, G. (2015) The molecular basis of oligomeric organization of the human m3 muscarinic acetylcholine receptor. Molecular Pharmacology, 87(6), pp. 936-953. (doi: 10.1124/mol.114.096925) (PMID:25769304)

Ward, R. J., Pediani, J. D. , Godin, A. G. and Milligan, G. (2015) Regulation of oligomeric organization of the serotonin 5-hydroxytryptamine 2C (5-HT2C) receptor observed by spatial intensity distribution analysis. Journal of Biological Chemistry, 290(20), pp. 12844-12857. (doi: 10.1074/jbc.M115.644724) (PMID:25825490) (PMCID:PMC4432300)

Divorty, N., Mackenzie, A., Nicklin, S. and Milligan, G. (2015) G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease. Frontiers in Pharmacology, 6, 41. (doi: 10.3389/fphar.2015.00041) (PMID:25805994) (PMCID:PMC4354270)

Hudson, B. D. , Christiansen, E., Murdoch, H., Jenkins, L. , Hansen, A. H., Madsen, O., Ulven, T. and Milligan, G. (2014) Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands. Molecular Pharmacology, 86(2), pp. 200-210. (doi: 10.1124/mol.114.093294)

Hudson, B. D. , Shimpukade, B., Milligan, G. and Ulven, T. (2014) The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120). Journal of Biological Chemistry, 289, pp. 20345-20358. (doi: 10.1074/jbc.M114.561449) (PMID:24860101) (PMCID:PMC4106347)

Zakrys, L., Ward, R. J., Pediani, J. D. , Godin, A. G., Graham, G. J. and Milligan, G. (2014) Roundabout 1 exists predominantly as a basal dimeric complex and this is unaffected by binding of the ligand Slit2. Biochemical Journal, 461(1), pp. 61-73. (doi: 10.1042/BJ20140190)

Butcher, A. J., Hudson, B. D. , Shimpukade, B., Alvarez-Curto, E. , Prihandoko, R., Ulven, T., Milligan, G. and Tobin, A. B. (2014) Concomitant action of structural elements and receptor phosphorylation determine arrestin-3 interaction with the free fatty acid receptor FFA4. Journal of Biological Chemistry, 289, pp. 18451-18465. (doi: 10.1074/jbc.M114.568816) (PMID:24817122) (PMCID:PMC4140278)

Fjaere, E. et al. (2014) Indomethacin treatment prevents high fat diet-induced obesity and insulin resistance but not glucose intolerance in C57BL/6J mice. Journal of Biological Chemistry, 289(23), pp. 16032-16045. (doi: 10.1074/jbc.M113.525220)

McKinney, C. A., Fattah, C., Loughrey, C. M. , Milligan, G. and Nicklin, S. A. (2014) Angiotensin-(1-7) and angiotensin-(1-9): function in cardiac and vascular remodeling. Clinical Science, 126, pp. 815-827. (doi: 10.1042/CS20130436)

Milligan, G. , Ulven, T., Murdoch, H. and Hudson, B. D. (2014) G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets. British Journal of Nutrition, 111(S1), S3-S7. (doi: 10.1017/S0007114513002249)

Ferre, S., Casado, V., Devi, L. A., Filizola, M., Jockers, R., Lohse, M. J., Milligan, G. , Pin, J.-P. and Guitart, X. (2014) G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives. Pharmacological Reviews, 66(2), pp. 413-434. (doi: 10.1124/pr.113.008052)

Ward, R.J. and Milligan, G. (2014) Structural and biophysical characterisation of G protein-coupled receptor ligand binding using resonance energy transfer and fluorescent labelling techniques. Biochimica et Biophysica Acta: Biomembranes, 1838(1A), pp. 3-14. (doi: 10.1016/j.bbamem.2013.04.007)

Mackenzie, A.E. et al. (2014) The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat gpr35. Molecular Pharmacology, 85(1), pp. 91-104. (doi: 10.1124/mol.113.089482)

Watterson, K. R., Hudson, B. D. , Ulven, T. and Milligan, G. (2014) Treatment of type 2 diabetes by free fatty acid receptor agonists. Frontiers in Endocrinology, 5, 137. (doi: 10.3389/fendo.2014.00137) (PMID:25221541) (PMCID:PMC4147718)

Horobin, R.W. , Rashid-Doubell, F., Pediani, J.D. and Milligan, G. (2013) Predicting small molecule fluorescent probe localization in living cells using QSAR modeling. 1. Overview and models for probes of structure, properties and function in single cells. Biotechnic and Histochemistry, 88(8), pp. 440-460. (doi: 10.3109/10520295.2013.780634)

Hudson, B.D. , Shimpukade, B., Mackenzie, A.E., Butcher, A.J., Pediani, J.D. , Christiansen, E., Heathcote, H., Tobin, A.B., Ulven, T. and Milligan, G. (2013) The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism. Molecular Pharmacology, 84(5), pp. 710-725. (doi: 10.1124/mol.113.087783)

Perez-Aso, M., Segura, V., Montó, F., Barettino, D., Noguera, M.A., Milligan, G. and D'Ocon, P. (2013) The three α₁-adrenoceptor subtypes show different spatio-temporal mechanisms of internalization and ERK1/2 phosphorylation. Biochimica et Biophysica Acta: Molecular Cell Research, 1833(10), pp. 2322-2333. (doi: 10.1016/j.bbamcr.2013.06.013)

Scott, E., Loya, K., Mountford, J., Milligan, G. and Baker, A. H. (2013) MicroRNA regulation of endothelial homeostasis and commitment—implications for vascular regeneration strategies using stem cell therapies. Free Radical Biology and Medicine, 64, pp. 52-60. (doi: 10.1016/j.freeradbiomed.2013.04.037)

Hudson, B.D. , Murdoch, H. and Milligan, G. (2013) The effects of species ortholog and SNP variation on receptors for free fatty acids. Molecular Endocrinology, 27(8), pp. 1177-1187. (doi: 10.1210/me.2013-1085)

Milligan, G. (2013) The prevalence, maintenance, and relevance of G protein-coupled receptor oligomerization. Molecular Pharmacology, 84(1), pp. 158-169. (doi: 10.1124/mol.113.084780)

Hudson, B.D. et al. (2013) Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor. Journal of Biological Chemistry, 288(24), pp. 17296-17312. (doi: 10.1074/jbc.M113.455337)

Christiansen, E. et al. (2013) Discovery of TUG-770: a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes. ACS Medicinal Chemistry Letters, 4(5), pp. 441-445. (doi: 10.1021/ml4000673)

Neetoo-Isseljee, Z., MacKenzie, A.E., Southern, C., Jerman, J., McIver, E. G., Harries, N., Taylor, D. L. and Milligan, G. (2013) High-throughput identification and characterization of novel, species-selective GPR35 agonists. Journal of Pharmacology and Experimental Therapeutics, 344(3), pp. 568-578. (doi: 10.1124/jpet.112.201798)

Christiansen, E. et al. (2013) Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability. Journal of Medicinal Chemistry, 56(3), pp. 982-992. (doi: 10.1021/jm301470a)

Clarke, C., Flores-Muñoz, M., McKinney, C. A., Milligan, G. and Nicklin, S. A. (2013) Regulation of cardiovascular remodeling by the counter-regulatory axis of the renin–angiotensin system. Future Cardiology, 9(1), pp. 23-38. (doi: 10.2217/fca.12.75)

Howard, L., MacKenzie, R. M., Pchelintsev, N. A., McBryan, T., McClure, J. D. , McBride, M. W. , Kane, N. M., Adams, P. D., Milligan, G. and Baker, A. H. (2013) Profiling of transcriptional and epigenetic changes during directed endothelial differentiation of human embryonic stem cells identifies FOXA2 as a marker of early mesoderm commitment. Stem Cell Research and Therapy, 4(2), Art. 36. (doi: 10.1186/scrt192)

Hudson, B. D. , Ulven, T. and Milligan, G. (2013) The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs. Current Topics in Medicinal Chemistry, 13(1), pp. 14-25. (doi: 10.2174/1568026611313010004)

Jenkins, L. , Harries, N., Lappin, J.E., MacKenzie, A.E., Neetoo-Isseljee, Z., Southern, C., McIver, E.G., Nicklin, S.A. , Taylor, D.L. and Milligan, G. (2013) Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. Journal of Pharmacology and Experimental Therapeutics, 343(3), pp. 683-695. (doi: 10.1124/jpet.112.198945) (PMID:22967846) (PMCID:PMC3500541)

Mackenzie, A. E., Neetoo-Isseljee, Z., Southern, C., Jerman, J., McIver, E. G., Hudson, B. D. , Taylor, D. L. and Milligan, G. (2013) Novel and potent GPR35 agonists aid identification of residues important in ligand interaction. FASEB Journal, 27, 655.1.

Patowary, S., Alvarez-Curto, E. , Xu, T.-R., Holz, J.D., Oliver, J.A., Milligan, G. and Raicu, V. (2013) The muscarinic M3acetylcholine receptor exists as two differently sized complexes at the plasma membrane. Biochemical Journal, 452(2), pp. 303-312. (doi: 10.1042/BJ20121902) (PMID:23521066)

Segura, V., Pérez-Aso, M., Montó, F., Carceller, E., Noguera, M.A., Pediani, J. , Milligan, G. , McGrath, I.C. and D’Ocon, P. (2013) Differences in the signaling pathways of α1A- and α1B-adrenoceptors are related to different endosomal targeting. PLoS ONE, 8(5), e64996. (doi: 10.1371/journal.pone.0064996) (PMID:23717684) (PMCID:PMC3663791)

Ward, R.W., Xu, T.-X. and Milligan, G. (2013) GPCR oligomerization and receptor trafficking. Methods in Enzymology, 521, pp. 69-90. (doi: 10.1016/B978-0-12-391862-8.00004-1)

Moreno, J.L. et al. (2012) Identification of three residues essential for 5-hydroxytryptamine 2A-metabotropic glutamate 2 (5-HT2A{middle dot}mGlu2) receptor heteromerization and its psychoactive behavioral function. Journal of Biological Chemistry, 287(53), pp. 44301-44319. (doi: 10.1074/jbc.M112.413161)

Hudson, B. , Christiansen, E., Tikhonova, I.G., Grundmann, M., Kostenis, E., Adams, D.R., Ulven, T. and Milligan, G. (2012) Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs. FASEB Journal, 26(12), pp. 4951-4965. (doi: 10.1096/fj.12-213314)

Hudson, B.D. , Tikhonova, I.G., Pandey, S.K., Ulven, T. and Milligan, G. (2012) Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3. Journal of Biological Chemistry, 287(49), pp. 41195-41209. (doi: 10.1074/jbc.M112.396259)

Christiansen, E. et al. (2012) Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. Journal of Medicinal Chemistry, 55(14), pp. 6624-6628. (doi: 10.1021/jm3002026)

Cunningham, M. R., McIntosh, K. A., Pediani, J. D. , Robben, J., Cooke, A. E., Nilsson, M., Gould, G. W. , Mundell, S., Milligan, G. and Plevin, R. (2012) Novel role for proteinase-activated receptor 2 (PAR2) in membrane trafficking of proteinase-activated receptor 4 (PAR4). Journal of Biological Chemistry, 287(20), pp. 16656-16669. (doi: 10.1074/jbc.M111.315911)

Shimpukade, B., Hudson, B.D. , Hogaard, C.K., Milligan, G. and Ulven, T. (2012) Discovery of a potent and selective GPR120 agonist. Journal of Medicinal Chemistry, 55(9), pp. 4511-4515. (doi: 10.1021/jm300215x)

Xu, T.-R., Ward, R. J., Pediani, J. D. and Milligan, G. (2012) Intramolecular fluorescence resonance energy transfer (FRET) sensors of the orexin OX1 and OX2 receptors identify slow kinetics of agonist activation. Journal of Biological Chemistry, 287, pp. 14937-14949. (doi: 10.1074/jbc.M111.334300)

Kane, N. M. et al. (2012) Role of MicroRNAs 99b, 181a, and 181b in the differentiation of human embryonic stem cells to vascular endothelial cells. Stem Cells, 30(4), pp. 643-654. (doi: 10.1002/stem.1026)

White, K., Kane, N. M., Milligan, G. and Baker, A. H. (2012) The role of miRNA in stem cell pluripotency and commitment to the vascular endothelial lineage. Microcirculation, 19(3), pp. 196-207. (doi: 10.1111/j.1549-8719.2012.00161.x)

Xu, T.-R., Lu, R.-F., Romano, D., Pitt, A., Houslay, M. D., Milligan, G. and Kolch, W. (2012) Eukaryotic translation initiation factor 3, subunit a, regulates the extracellular signal-regulated kinase pathway. Molecular and Cellular Biology, 32(1), pp. 88-95. (doi: 10.1128/​MCB.05770-11)

Flores, M., Graham, D. , Dominiczak, A.F. , Milligan, G. , Baker, A.H. and Nicklin, S.A. (2012) Angiotensin-(1-9) antagonises Angiotensin II-induced cardiac remodeling via the angiotensin type 2 receptor. Proceedings of the Physiological Society, 27, C1.

Flores, M., Graham, D. , Dominiczak, A. F. , Milligan, G. , Baker, A. H. and Nicklin, S. A. (2012) Abstract 231: angiotensin-(1-9) antagonises cardiac remodelling in a mouse model of Angiotensin Ii-induced hypertension. Hypertension, 60, A231.

Georgoussi, Z., Georganta, E.M. and Milligan, G. (2012) The other side of opioid receptor signalling: regulation by protein-protein interaction. Current Drug Targets, 13(1), pp. 80-102. (doi: 10.2174/138945012798868470)

Laarman, A.J. et al. (2012) Staphylococcus aureus Staphopain A inhibits CXCR2-dependent neutrophil activation and chemotaxis. EMBO Journal, 31(17), pp. 3607-3619. (doi: 10.1038/emboj.2012.212)

Pou, C., Mannoury la Cour, C., Stoddart, L.A., Millan, M.J. and Milligan, G. (2012) Functional homomers and heteromers of dopamine D_2L and D₃ receptors co-exist at the cell surface. Journal of Biological Chemistry, 287(12), pp. 8864-8878. (doi: 10.1074/jbc.M111.326678)

Terhzaz, S. , Cabrero, P. , Robben, J.H., Radford, J.C., Hudson, B.D. , Milligan, G. , Dow, J.A.T. and Davies, S.A. (2012) Mechanism and function of drosophila capa GPCR: a desiccation stress-responsive receptor with functional homology to human neuromedinU receptor. PLoS ONE, 7(1), e29897. (doi: 10.1371/journal.pone.0029897) (PMID:22253819) (PMCID:PMC3256212)

Mackenzie, A.E., Lappin, J.E., Taylor, D.L., Nicklin, S.A. and Milligan, G. (2011) GPR35 as a novel therapeutic target. Frontiers in Endocrinology, 2, 68. (doi: 10.3389/fendo.2011.00068) (PMID:22654822) (PMCID:PMC3356001)

Alvarez-Curto, E. , Prihandoko, R., Tautermann, C. S., Zwier, J. M., Pediani, J. D. , Lohse, M. J., Hoffmann, C., Tobin, A. B. and Milligan, G. (2011) Developing chemical genetic approaches to explore G protein-coupled receptor function: validation of the use of a Receptor Activated Solely by Synthetic Ligand (RASSL). Molecular Pharmacology, 80(6), pp. 1033-1046. (doi: 10.1124/mol.111.074674) (PMID:21880827) (PMCID:PMC3228535)

Ward, R. J., Pediani, J. D. and Milligan, G. (2011) Heteromultimerization of cannabinoid CB₁ receptor and orexin OX₁ receptor generates a unique complex in which both protomers are regulated by orexin A. Journal of Biological Chemistry, 286(43), pp. 37414-37428. (doi: 10.1074/jbc.M111.287649)

Howard, L., Kane, N., Milligan, G. and Baker, A. H. (2011) MicroRNAs regulating cell pluripotency and vascular differentiation. Vascular Pharmacology, 55(4), pp. 69-78. (doi: 10.1016/j.vph.2011.08.002)

Xu, T.‑R., Ward, R. J., Pediani, J. D. and Milligan, G. (2011) The orexin OX₁ receptor exists predominantly as a homodimer in the basal state: potential regulation of receptor organization by both agonist and antagonist ligands. Biochemical Journal, 439(1), pp. 171-183. (doi: 10.1042/BJ20110230)

Van Lith, M., Tiwari, S., Pediani, J. , Milligan, G. and Bulleid, N. J. (2011) Real-time monitoring of redox changes in the mammalian endoplasmic reticulum. Journal of Cell Science, 124(14), pp. 2349-2356. (doi: 10.1242/jcs.085530)

Smith, N.J. et al. (2011) Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. Molecular Pharmacology, 80(1), pp. 163-173. (doi: 10.1124/mol.110.070789)

Nejsum, L.N., Christensen, T.M., Robben, J.H., Milligan, G. , Deen, P.M.T., Bichet, D.G. and Levin, K. (2011) Novel mutation in the AVPR2 gene in a Danish male with nephrogenic diabetes insipidus caused by ER retention and subsequent lysosomal degradation of the mutant receptor. NDT Plus, 4(3), pp. 158-163. (doi: 10.1093/ndtplus/sfr010) (PMID:21629670) (PMCID:PMC3103721)

Schmidt, J. et al. (2011) Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. Journal of Biological Chemistry, 286(12), pp. 10628-10640. (doi: 10.1074/jbc.M110.210872)

Anthony, D.F., Sin, Y.Y. , Vadrevu, S., Advant, N., Day, J.P., Byrne, A.M., Lynch, M.J., Milligan, G. , Houslay, M.D. and Baillie, G.S. (2011) β-Arrestin 1 inhibits the GAP function of ARHGAP21 so as to promote the activation of RhoA following angiotensin II type 1A receptor stimulation. Molecular and Cellular Biology, 31(5), pp. 1066-1075. (doi: 10.1128/MCB.00883-10) (PMID:21173159) (PMCID:PMC3067824)

Ward, R. J., Pediani, J. D. and Milligan, G. (2011) Ligand-induced internalisation of the orexin OX1 and cannabinoid CB1 receptors assessed via N-terminal SNAP and CLIP-tagging. British Journal of Pharmacology, 162(6), pp. 1439-1452. (doi: 10.1111/j.1476-5381.2010.01156.x)

Flores-Munoz, M., Smith, N. J., Haggerty, C., Milligan, G. and Nicklin, S. A. (2011) Angiotensin1-9 antagonises pro-hypertrophic signalling in cardiomyocytes via the angiotensin type 2 receptor. Journal of Physiology, 589(4), pp. 939-951. (doi: 10.1113/jphysiol.2010.203075)

Smith, N.J., Bennett, K. and Milligan, G. (2011) When simple agonism is not enough: Emerging modalities of GPCR ligands. Molecular and Cellular Endocrinology, 331(2), pp. 241-247. (doi: 10.1016/j.mce.2010.07.009)

Dimond, P. et al. (2011) G protein-coupled receptor modulation with pepducins: moving closer to the clinic. Annals of the New York Academy of Sciences, 1226(1), pp. 34-49. (doi: 10.1111/j.1749-6632.2011.06039.x)

Milligan, G. (2011) Orthologue selectivity and ligand bias: translating the pharmacology of GPR35. Trends in Pharmacological Sciences, 32(5), pp. 317-325. (doi: 10.1016/j.tips.2011.02.002)

Schröder, R. et al. (2011) Applying label-free dynamic mass redistribution technology to frame signaling of G protein–coupled receptors noninvasively in living cells. Nature Protocols, 6(11), pp. 1748-1760. (doi: 10.1038/nprot.2011.386)

Tarrasón, G. et al. (2011) The sphingosine-1-phosphate receptor-1 antagonist, W146, causes early and short-lasting peripheral blood lymphopenia in mice. International Immunopharmacology, 11(11), pp. 1773-1779. (doi: 10.1016/j.intimp.2011.07.004)

Ward, R.J., Alvarez-Curto, E. and Milligan, G. (2011) Using the Flp-In™ T-Rex™ System to Regulate GPCR Expression. Methods in Molecular Biology, 746, pp. 21-37. (doi: 10.1007/978-1-61779-126-0_2)

Burton, P. et al. (2010) Erythro-9-(2-hydroxy-3-nonyl)adenine (EHNA) blocks differentiation and maintains the expression of pluripotency markers in human embryonic stem cells. Biochemical Journal, 432(3), pp. 575-584. (doi: 10.1042/BJ20100726)

Kane, N. M. et al. (2010) Lentivirus-mediated reprogramming of somatic cells in the absence of transgenic transcription factors. Molecular Therapy, 18(12), pp. 2139-2145. (doi: 10.1038/mt.2010.231)

Smith, N. J. and Milligan, G. (2010) Allostery at G protein-coupled receptor Homo- and Heteromers: uncharted pharmacological landscapes. Pharmacological Reviews, 62(4), pp. 701-725. (doi: 10.1124/pr.110.002667) (PMID:21079041) (PMCID:PMC2993260)

Lopez-Gimenez, J.F. and Milligan, G. (2010) Opioid regulation of Mu receptor internalisation: relevance to the development of tolerance and dependence. CNS and Neurological Disorders: Drug Targets, 9(5), pp. 616-626. (doi: 10.2174/187152710793361522) (PMID:20632966)

Alvarez-Curto, E. , Pediani, J. D. and Milligan, G. (2010) Applications of fluorescence and bioluminescence resonance energy transfer to drug discovery at G protein coupled receptors. Analytical and Bioanalytical Chemistry, 398(1), pp. 167-180. (doi: 10.1007/s00216-010-3823-4) (PMID:20517598)

Schroder, R. et al. (2010) Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements. Nature Biotechnology, 28(9), pp. 943-949. (doi: 10.1038/nbt.1671)

Burton, P. et al. (2010) Identification and characterization of small-molecule ligands that maintain pluripotency of human embryonic stem cells. Biochemical Society Transactions, 38(4), pp. 1058-1061. (doi: 10.1042/BST0381058)

Alvarez-Curto, E., Ward, R. J., Pediani, J. D. and Milligan, G. (2010) Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogenous time-resolved FRET. Journal of Biological Chemistry, 285(30), pp. 23318-23330. (doi: 10.1074/jbc.M110.122184) (PMID:20489201) (PMCID:PMC2906324)

Khelashvili, G. et al. (2010) GPCR-OKB: the G protein coupled receptor oligomer knowledge base. Bioinformatics, 26(14), pp. 1804-1805. (doi: 10.1093/bioinformatics/btq264)

Kane, N. M., Meloni, M., Spencer, H. L., Craig, M. A., Strehl, R., Milligan, G., Houslay, M. D., Mountford, J. C., Emanueli, C. and Baker, A. H. (2010) Derivation of endothelial cells from human embryonic stem cells by directed differentiation: analysis of microRNA and angiogenesis in vitro and in vivo. Arteriosclerosis, Thrombosis, and Vascular Biology, 30(7), pp. 1389-1397. (doi: 10.1161/ATVBAHA.110.204800)

del Burgo, L. S. and Milligan, G. (2010) Heterodimerisation of G protein-coupled receptors: implications for drug design and ligand screening. Expert Opinion on Drug Discovery, 5(5), pp. 461-474. (doi: 10.1517/17460441003720467) (PMID:22823130)

Milligan, G. (2010) The role of dimerisation in the cellular trafficking of G-protein-coupled receptors. Current Opinion in Pharmacology, 10(1), pp. 23-29. (doi: 10.1016/j.coph.2009.09.010) (PMID:19850521)

Andrews, P. et al. (2010) High content screening of feeder-free human embryonic stem cells to identify pro-survival small molecules. Biochemical Journal, 432(Pt 1), pp. 21-33. (doi: 10.1042/BJ20101022)

Burton, P. et al. (2010) Identification and characterization of small-molecule ligands that maintain pluripotency of human embryonic stem cells. Biochemical Society Transactions, 38(4), pp. 1058-1061. (doi: 10.1042/BST0381058)

Jenkins, L. , Alvarez-Curto, E. , Campbell, K., De Munnik, S., Canals Buj, M., Schlyer, S. and Milligan, G. (2010) Agonist activation of the G protein-coupled receptor GPR35 involves transmembrane domain III and is transduced via Gα13 and β-arrestin-2. British Journal of Pharmacology, 162(3), pp. 733-748. (doi: 10.1111/j.1476-5381.2010.01082.x)

Jenkins, L. , Brea, J., Smith, N.J., Hudson, B.D. , Reilly, G., Bryant, N.J., Castro, M., Loza, M.I. and Milligan, G. (2010) Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13. Biochemical Journal, 432(3), pp. 451-459. (doi: 10.1042/BJ20101287)

Stoddart, L.A. and Milligan, G. (2010) Constitutive activity of GPR40/FFA1 intrinsic or assay dependent? Methods in Enzymology, 484, pp. 569-590. (doi: 10.1016/B978-0-12-381298-8.00028-9) (PMID:21036251)

Xu, T. et al. (2010) Inferring signaling pathway topologies from multiple perturbation measurements of specific biochemical species. Science Signaling, 3(113), ra20. (doi: 10.1126/scisignal.2000517)

Robben, J.H., Fenton, R.A., Vargas, S.L., Schweer, H., Peti-Peterdi, J., Deen, P.M.T. and Milligan, G. (2009) Localization of the succinate receptor in the distal nephron and its signaling in polarized MDCK cells. Kidney International, 76(12), pp. 1258-1267. (doi: 10.1038/ki.2009.360)

Milligan, G. (2009) G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function. British Journal of Pharmacology, 158(1), pp. 5-14. (doi: 10.1111/j.1476-5381.2009.00169.x) (PMID:19309353) (PMCID:PMC2795239)

Milligan, G. and McGrath, J.C. (2009) GPCR theme editorial. British Journal of Pharmacology, 158(1), pp. 1-4. (doi: 10.1111/j.1476-5381.2009.00422.x)

Robben, J.H., Kortenoeven, M.L.A., Sze, M., Yae, C., Milligan, G. , Oorschot, V.M., Klumperman, J., Knoers, N.V.A.M. and Deen, P.M.T. (2009) Intracellular activation of vasopressin V2 receptor mutants in nephrogenic diabetes insipidus by nonpeptide agonists. Proceedings of the National Academy of Sciences of the United States of America, 106(29), pp. 12195-12200. (doi: 10.1073/pnas.0900130106)