Professor Harry De Koning

Professor of Parasite Biochemistry and Pharmacology (Parasitology)

telephone: 01413303753
email: Harry.De-Koning@glasgow.ac.uk

RB518 Level B5, Iii - Gbrc, University Place, Glasgow G12 8TA

Research interests

The two main aspects of my research are the investigation of the mechanisms of drug resistance in protozoan parasites, mainly African trypanosomes, and the identification of new lead compounds and therapeutic strategies against various protozoan pathogens including Trypanosoma brucei, Trypanosoma congolense, Leishmania species and Trichomonas vaginalis.

The two most important classes of drugs against African trypanosomiasis in humans (also called sleeping sickness) and animals are commonly known as aromatic diamidines and melaminophenyl arsenicals. Both classes of drugs are old, dating from the 1930s and their long usage has inevitably led to highly significant levels of resistance in the parasites. We have investigated the mechanisms by which the trypanosomes become resistant to the drugs and found this is mostly linked to the loss of specific transport proteins; in their absence the drugs do not enter the parasite and are therefore ineffective. We have identified and characterised these transporters and ongoing work is identifying the genes encoding them so that genetic research can be performed on parasite populations. We further work on the identification of the Trypanosoma brucei resistance mechanism for isometamidium, an important phenanthridine drug against animal trypanosomiasis in sub-Saharan Africa.

We have developed much needed screening tools for drug efficacy to some parasites, including Leishmania species, Trypanosoma species and Trichomonas vaginalis. These enable the screening of compound collections for activity against these pathogens. We are working together with academic collaborators and pharmaceutical companies to discover new lead compounds for pre-clinical drug development. Several series of compounds have been tested and promising leads have been identified, especially against Trypanosoma species.

Finally, our emphasis on transporters of protozoan parasites is not limited to drug transporters per se. I have worked on nutrient transporters, particularly purine and pyrimidine transporters since 1994 and contributed much to our knowledge how protozoa take up these vital nutrients from their hosts. Having recently characterised pyrimidine transport activities in several protozoa, current projects include the identification of pyrimidine transporter genes in Trypanosoma and Leishmania species, and the characterisation of nucleoside and nucleobase transporters in Trichomonas vaginalis.

Publications

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Number of items: 193.

2024

Oaikhena, E. E. et al. (2024) The activities of suaveolol and other compounds from Hyptis suaveolens and Momordica charantia against the aetiological agents of African trypanosomiasis, leishmaniasis and malaria. Experimental Parasitology, 263-64, 108807. (doi: 10.1016/j.exppara.2024.108807) (PMID:39043327)

Ungogo, M. A. and de Koning, H. P. (2024) Drug resistance in animal trypanosomiases: Epidemiology, mechanisms and control strategies. International Journal for Parasitology: Drugs and Drug Resistance, 25, 100533. (doi: 10.1016/j.ijpddr.2024.100533) (PMID:38555795) (PMCID:PMC10990905)

Aldfer, M. M. , Hulpia, F., van Calenbergh, S. and De Koning, H. P. (2024) Mapping the transporter-substrate interactions of the Trypanosoma cruzi NB1 nucleobase transporter reveals the basis for its high affinity and selectivity for hypoxanthine and guanine and lack of nucleoside uptake. Molecular and Biochemical Parasitology, 258, 111616. (doi: 10.1016/j.molbiopara.2024.111616) (PMID:38401850)

2023

Elati, H. A.A. , Goerner, A. L., Martorelli Di Genova, B., Sheiner, L. and De Koning, H. P. (2023) Pyrimidine salvage in Toxoplasma gondii as a target for new treatment. Frontiers in Cellular and Infection Microbiology, 13, 1320160. (doi: 10.3389/fcimb.2023.1320160) (PMID:38162577) (PMCID:PMC10755004)

Bachmaier, S., Gould, M. K., Polatoglou, E., Omelianczyk, R., Brennand, A. E., Aloraini, M. A., Munday, J. C. , Horn, D., Boshart, M. and De Koning, H. (2023) Novel kinetoplastid-specific cAMP binding proteins identified by RNAi screening for cAMP resistance in T. brucei. Frontiers in Cellular and Infection Microbiology, 13, 1204707. (doi: 10.3389/fcimb.2023.1204707) (PMID:37475965) (PMCID:PMC10354285)

Timm, B. L., da Gama, A. N. S., Batista, M. M., Batista, D. d. G. J., Boykin, D. W., De Koning, H. P. and Correia Soeiro, M. d. N. (2023) Arylimidamides have potential for chemoprophylaxis against blood-transmitted Chagas disease. Pathogens, 12(5), 701. (doi: 10.3390/pathogens12050701) (PMID:37242371) (PMCID:PMC10224031)

Ungogo, M. A. et al. (2023) Cloning and characterization of Trypanosoma congolense and T. vivax nucleoside transporters reveal the potential of P1-type carriers for the discovery of broad-spectrum nucleoside-based therapeutics against Animal African Trypanosomiasis. International Journal of Molecular Sciences, 24(4), 3144. (doi: 10.3390/ijms24043144) (PMID:36834557) (PMCID:PMC9960827)

Alenezi, S. S. et al. (2023) The activity of red Nigerian propolis and some of its components against Trypanosoma brucei and Trypanosoma congolense. Molecules, 28(2), 622. (doi: 10.3390/molecules28020622) (PMID:36677679) (PMCID:PMC9860874)

2022

Aldfer, M. M. , Alfayez, I. A., Elati, H. A.A. , Gayen, N., Elmahallawy, E. K., Murillo, A. M., Marsiccobetre, S., Van Calenbergh, S., Siber, A. M. and De Koning, H. P. (2022) The Trypanosoma cruzi TcrNT2 nucleoside transporter is a conduit for the uptake of 5-F-2’-deoxyuridine and tubercidin analogues. Molecules, 27(22), 8045. (doi: 10.3390/molecules27228045) (PMID:36432150) (PMCID:PMC9693223)

Fiuza, L. F. d. A. et al. (2022) Phenotypic evaluation of nucleoside analogues against Trypanosoma cruzi infection: in vitro and in vivo approaches. Molecules, 27(22), 8087. (doi: 10.3390/molecules27228087) (PMID:36432189) (PMCID:PMC9695592)

Jansen, E. E.L., de Kok, I. M.C.M., Kaljouw, S., Demirel, E., De Koning, H. J. and Hontelez, J. A.C. (2022) Rapid elimination of cervical cancer while maintaining the harms and benefits ratio of cervical cancer screening: a modelling study. BMC Medicine, 20(1), 433. (doi: 10.1186/s12916-022-02631-7) (PMID:36352410) (PMCID:PMC9645325)

Sartania, N. , Sneddon, S. , Boyle, J. G., McQuarrie, E. and de Koning, H. P. (2022) Increasing collaborative discussion in case-based learning improves student engagement and knowledge acquisition. Medical Science Educator, 32(5), pp. 1055-1064. (doi: 10.1007/s40670-022-01614-w) (PMID:36276760) (PMCID:PMC9584010)

Balogun, J. B. et al. (2022) Prevalence and associated risk factors of urinary schistosomiasis among primary school pupils in the Jidawa and Zobiya communities of Jigawa State, Nigeria. Annals of Global Health, 88(1), 71. (doi: 10.5334/aogh.3704) (PMID:36062044) (PMCID:PMC9389954)

Aldfer, M. M. , AlSiari, T. A., Elati, H. A.A. , Natto, M. J., Alfayez, I. A., Campagnaro, G. D., Sani, B., Burchmore, R. J. S. , Diallinas, G. and De Koning, H. (2022) Nucleoside transport and nucleobase uptake null mutants in Leishmania mexicana for the routine expression and characterization of purine and pyrimidine transporters. International Journal of Molecular Sciences, 23(15), 8139. (doi: 10.3390/ijms23158139) (PMID:35897714) (PMCID:PMC9331716)

Mabille, D., Ilbeigi, K., Hendrickx, S., Ungogo, M. A., Hulpia, F., Lin, C., Maes, L., de Koning, H. P. , Van Calenbergh, S. and Caljon, G. (2022) Nucleoside analogues for the treatment of animal trypanosomiasis. International Journal for Parasitology: Drugs and Drug Resistance, 19, pp. 21-30. (doi: 10.1016/j.ijpddr.2022.05.001) (PMID:35567803) (PMCID:PMC9111543)

Alenezi, S. S. et al. (2022) The antiprotozoal activity of Papua New Guinea propolis and its triterpenes. Molecules, 27(5), 1622. (doi: 10.3390/molecules27051622) (PMID:35268726) (PMCID:PMC8911803)

Ungogo, M. A., Campagnaro, G. D., Alghamdi, A. H., Natto, M. J. and de Koning, H. P. (2022) Differences in transporters rather than drug targets are the principal determinants of the different innate sensitivities of Trypanosoma congolense and Trypanozoon subgenus trypanosomes to diamidines and melaminophenyl arsenicals. International Journal of Molecular Sciences, 23(5), 2844. (doi: 10.3390/ijms23052844) (PMID:35269985) (PMCID:PMC8911344)

Cisneros, D. et al. (2022) Imidazoline- and benzamidine-based trypanosome alternative oxidase inhibitors: synthesis and structure–activity relationship studies. ACS Medicinal Chemistry Letters, 13(2), pp. 312-318. (doi: 10.1021/acsmedchemlett.1c00717) (PMID:35178188) (PMCID:PMC8842630)

Campagnaro, G. D., Elati, H. A. A. , Balaska, S., Martin Abril, M. E., Natto, M. J., Hulpia, F., Lee, K., Sheiner, L. , Van Calenbergh, S. and de Koning, H. P. (2022) A Toxoplasma gondii oxopurine transporter binds nucleobases and nucleosides using different binding modes. International Journal of Molecular Sciences, 23(2), 710. (doi: 10.3390/ijms23020710) (PMID:35054895) (PMCID:PMC8776092)

2021

Natto, M. J., Miyamoto, Y., Munday, J. C. , AlSiari, T. A., Al-Salabi, M. I., Quashie, N. B., Eze, A. A., Eckmann, L. and De Koning, H. P. (2021) Comprehensive characterisation of purine and pyrimidine transport activities in Trichomonas vaginalis and functional cloning of a trichomonad nucleoside transporter. Molecular Microbiology, 116(6), pp. 1489-1511. (doi: 10.1111/mmi.14840) (PMID:34738285)

Burley, G., Watson, A. J. B., de Koning, H. , Jones, K., Robertson, J., Bode, B., McWhinnie, F., Ungogo, M., Aldfer, M. and Lemgruber Soares, L. (2021) Direct, late‐stage mono‐N‐arylation of pentamidine: method development, mechanistic insights, and expedient access to novel antiparastitics against diamidine‐resistant parasites. ChemMedChem, 16(22), pp. 3396-3401. (doi: 10.1002/cmdc.202100509) (PMID:34357687)

Cueto-Díaz, E. J. et al. (2021) Synthesis, biological, and photophysical studies of molecular rotor-based fluorescent inhibitors of the Trypanosome Alternative Oxidase. European Journal of Medicinal Chemistry, 2020, 113470. (doi: 10.1016/j.ejmech.2021.113470) (PMID:33940464)

Carruthers, L. V. et al. (2021) Diminazene resistance in Trypanosoma congolense is not caused by reduced transport capacity but associated with reduced mitochondrial membrane potential. Molecular Microbiology, 116(2), pp. 564-588. (doi: 10.1111/mmi.14733) (PMID:33932053)

Alotaibi, A. et al. (2021) Activity of compounds from temperate propolis against Trypanosoma brucei and Leishmania mexicana. Molecules, 26(13), 3912. (doi: 10.3390/molecules26133912) (PMID:34206940) (PMCID:PMC8272135)

Steketee, P. C. et al. (2021) Divergent metabolism between Trypanosoma congolense and Trypanosoma brucei results in differential sensitivity to metabolic inhibition. PLoS Pathogens, 17(7), e1009734. (doi: 10.1371/journal.ppat.1009734) (PMID:34310651) (PMCID:PMC8384185)

Natto, M. J., Hulpia, F., Kalkman, E. R., Baillie, S., Alhejely, A., Miyamoto, Y., Eckmann, L., Van Calenbergh, S. and de Koning, H. P. (2021) Deazapurine nucleoside analogues for the treatment of Trichomonas vaginalis. ACS Infectious Diseases, 7(6), pp. 1752-1764. (doi: 10.1021/acsinfecdis.1c00075) (PMID:33974405)

Anyam, J. V., Daikwo, P. E., Ungogo, M. A., Nweze, N. E., Igoli, N. P., Gray, A. I., De Koning, H. P. and Igoli, J. O. (2021) Two new antiprotozoal diterpenes from the roots of Acacia nilotica. Frontiers in Chemistry, 9, 624741. (doi: 10.3389/fchem.2021.624741) (PMID:33968894) (PMCID:PMC8097170)

de Araújo, J. S. et al. (2021) A tetrahydrophthalazinone inhibitor of phosphodiesterase with in vitro activity against intracellular trypanosomatids. Antimicrobial Agents and Chemotherapy, 65(3), e00960-20. (doi: 10.1128/AAC.00960-20) (PMID:33361300) (PMCID:PMC8092546)

Zheoat, A. M., Alenezi, S., Elmahallawy, E. K., Ungogo, M. A., Alghamdi, A. H., Watson, D. G., Igoli, J. O., Gray, A. I., de Koning, H. P. and Ferro, V. A. (2021) Antitrypanosomal and antileishmanial activity of chalcones and flavanones from Polygonum salicifolium. Pathogens, 10(2), 175. (doi: 10.3390/pathogens10020175) (PMID:33562567) (PMCID:PMC7915666)

Alkhaldi, A. A.M., De Koning, H. P. and Bukhari, S. N. A. (2021) Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes. Brazilian Journal of Pharmaceutical Sciences, 57, e18997. (doi: 10.1590/s2175-97902020000418997)

2020

Ungogo, M. A., Ebiloma, G. U., Ichoron, N., Igoli, J. O., De Koning, H. P. and Balogun, E. O. (2020) A review of the antimalarial, antitrypanosomal, and antileishmanial activities of natural compounds isolated from Nigerian flora. Frontiers in Chemistry, 8, 617448. (doi: 10.3389/fchem.2020.617448) (PMID:33425860) (PMCID:PMC7786139)

Alenezi, S. S., Natto, M. J., Igoli, J. O., Gray, A. I., Fearnley, J., Fearnley, H., De Koning, H. P. and Watson, D. G. (2020) Novel flavanones with anti-trypanosomal activity isolated from Zambian and Tanzanian propolis samples. International Journal for Parasitology: Drugs and Drug Resistance, 14, pp. 201-207. (doi: 10.1016/j.ijpddr.2020.10.011) (PMID:33160277) (PMCID:PMC7649109)

Nvau, J. B., Alenezi, S., Ungogo, M. A., Alfayez, I. A.M., Natto, M. J., Gray, A. I., Ferro, V. A., Watson, D. G., De Koning, H. P. and Igoli, J. O. (2020) Antiparasitic and cytotoxic activity of bokkosin, a novel diterpene-substituted chromanyl benzoquinone from Calliandra portoricensis. Frontiers in Chemistry, 8, p. 574103. (doi: 10.3389/fchem.2020.574103) (PMID:33282826) (PMCID:PMC7705231)

Ebiloma, G. U., Ichoron, N., Siheri, W., Watson, D. G., Igoli, J. O. and De Koning, H. P. (2020) The strong anti-kinetoplastid properties of bee propolis: composition and identification of the active agents and their biochemical targets. Molecules, 25(21), 5155. (doi: 10.3390/molecules25215155) (PMID:33167520) (PMCID:PMC7663965)

Campagnaro, G. D. and De Koning, H. P. (2020) Purine and pyrimidine transporters of pathogenic protozoa – conduits for therapeutic agents. Medicinal Research Reviews, 40(5), pp. 1679-1714. (doi: 10.1002/med.21667) (PMID:32144812)

de Araújo, J. S. et al. (2020) Efficacy of novel pyrazolone phosphodiesterase inhibitors in experimental mouse models of Trypanosoma cruzi. Antimicrobial Agents and Chemotherapy, 64(9), e00414-20. (doi: 10.1128/AAC.00414-20) (PMID:32601163) (PMCID:PMC7449165)

Hulpia, F., Campagnaro, G. D., Alzahrani, K. J., Alfayez, I. A., Ungogo, M. A., Mabille, D., Maes, L., de Koning, H. P. , Caljon, G. and Van Calenbergh, S. (2020) Structure–activity relationship exploration of 3′-deoxy-7-deazapurine nucleoside analogues as anti-Trypanosoma brucei agents. ACS Infectious Diseases, 6(8), pp. 2045-2056. (doi: 10.1021/acsinfecdis.0c00105) (PMID:32568511)

Munday, J. C. et al. (2020) Cloning and functional complementation of ten Schistosoma mansoni phosphodiesterases expressed in the mammalian host stages. PLoS Neglected Tropical Diseases, 14(7), e0008447. (doi: 10.1371/journal.pntd.0008447) (PMID:32730343) (PMCID:PMC7430754)

Quintana, J. F. , Bueren-Calabuig, J., Zuccotto, F., de Koning, H. P. , Horn, D. and Field, M. C. (2020) Instability of aquaglyceroporin (AQP) 2 contributes to drug resistance in Trypanosoma brucei. PLoS Neglected Tropical Diseases, 14(7), e0008458. (doi: 10.1371/journal.pntd.0008458) (PMID:32644992) (PMCID:PMC7413563)

Zoltner, M. et al. (2020) Suramin exposure alters cellular metabolism and mitochondrial energy production in African trypanosomes. Journal of Biological Chemistry, 295(24), pp. 8331-8347. (doi: 10.1074/jbc.ra120.012355) (PMID:32354742) (PMCID:PMC7294092)

De Araújo, J. S. et al. (2020) Evaluation of phthalazinone phosphodiesterase inhibitors with improved activity and selectivity against Trypanosoma cruzi. Journal of Antimicrobial Chemotherapy, 75(4), pp. 958-967. (doi: 10.1093/jac/dkz516) (PMID:31860098)

Hulpia, F., Bouton, J., Campagnaro, G. D., Alfayez, I. A., Mabille, D., Maes, L., de Koning, H. P. , Caljon, G. and Van Calenbergh, S. (2020) C6–O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents. European Journal of Medicinal Chemistry, 188, 112018. (doi: 10.1016/j.ejmech.2019.112018) (PMID:31931339)

De Koning, H. P. (2020) The drugs of sleeping sickness: their mechanisms of action and resistance, and a brief history. Tropical Medicine and Infectious Disease, 5(1), 14. (doi: 10.3390/tropicalmed5010014)

Alkhaldi, A. A.M., Musa, A., Mostafa, E. M., Amin, E. and De Koning, H. P. (2020) Docking studies and antiprotozoal activity of secondary metabolites isolated from Scrophularia syriaca Benth. growing in Saudi Arabia. Records of Natural Products, 14(1), pp. 23-30. (doi: 10.25135/rnp.19.03.1224)

Botros, S. S., El-Lakkany, N. M., Seif el-Din, S. H., William, S., Sabra, A.-N., Hammam, O. A. and De Koning, H. P. (2020) The phosphodiesterase-4 inhibitor roflumilast impacts Schistosoma mansoni ovipositing in vitro but displays only modest antischistosomal activity in vivo. Experimental Parasitology, 208, 107793. (doi: 10.1016/j.exppara.2019.107793) (PMID:31711973)

Alghamdi, A. et al. (2020) Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei. eLife, 9, e56416. (doi: 10.7554/eLife.56416) (PMID:32762841) (PMCID:PMC7473772)

2019

Khandazhinskaya, A. L. et al. (2019) Investigation of 5’-norcarbocyclic nucleoside analogues as antiprotozoal and antibacterial agents. Molecules, 24(19), e3433. (doi: 10.3390/molecules24193433) (PMID:31546633)

De Heuvel, E. et al. (2019) Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors. Bioorganic and Medicinal Chemistry, 27(18), pp. 3998-4012. (doi: 10.1016/j.bmc.2019.06.027) (PMID:31327675)

Ebiloma, G. U., Balogun, E. O., Cueto-Díaz, E. J., de Koning, H. P. and Dardonville, C. (2019) Alternative oxidase inhibitors: mitochondrion-targeting as a strategy for new drugs against pathogenic parasites and fungi. Medicinal Research Reviews, 39(5), pp. 1553-1602. (doi: 10.1002/med.21560) (PMID:30693533)

Alotaibi, A., Ebiloma, G., Williams, R., Alanazi, S., Donachie, A. M., Guillaume, S., Igoli, J.O., Fearnley, J., De Koning, H. P. and Watson, D.G. (2019) European propolis is highly active against trypanosomatids including Crithidia fasciculata. Scientific Reports, 9, 11364. (doi: 10.1038/s41598-019-47840-y) (PMID:31388043) (PMCID:PMC6684629)

Sebastián-Pérez, V. et al. (2019) Discovery of novel Schistosoma mansoni PDE4A inhibitors as potential agents against schistosomiasis. Future Medicinal Chemistry, 11(14), pp. 1703-1720. (doi: 10.4155/fmc-2018-0592) (PMID:31370708)

Alkhaldi, A.A.M., De Koning, H.P. and Bukhari, S.N.A. (2019) Effects of some natural leads on Trypanosoma and Leishmania strains. Tropical Biomedicine, 36(2), pp. 373-378.

Alkhaldi, A. A.M., Abdelgawad, M. A., Youssif, B. G.M., El-Gendy, A. O. and De Koning, H. (2019) Synthesis, antimicrobial activities and GAPDH docking of new 1,2,3-triazole derivatives. Tropical Journal of Pharmaceutical Research, 18(5), 1108. (doi: 10.4314/tjpr.v18i5.27)

Alkhaldi, A. A., De Koning, H. P. and Bukhari, S. N. A. (2019) Antileishmanial and antitrypanosomal activity of symmetrical dibenzyl-substituted α,β-unsaturated carbonyl-based compounds. Drug Design, Development and Therapy, 13, pp. 1179-1185. (doi: 10.2147/DDDT.S204733) (PMID:31118564) (PMCID:PMC6500899)

Botros, S. S. et al. (2019) Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity. International Journal for Parasitology: Drugs and Drug Resistance, 9, pp. 35-43. (doi: 10.1016/j.ijpddr.2019.01.001)

Eze, A. A., Igoli, J., Gray, A. I., Skellern, G. G. and De Koning, H. P. (2019) The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance. International Journal for Parasitology: Drugs and Drug Resistance, 9, pp. 54-58. (doi: 10.1016/j.ijpddr.2019.01.003) (PMID:30685630) (PMCID:PMC6356087)

Siciliano de Araújo, J., Garcia-Rubia, A., Sebastian-Perez, V., Kalejaiye, T. D., Bernardino da Silva, P., Fonseca-Berzal, C. R., Maes, L., De Koning, H. P. , de Nazaré Correia Soeiroa, M. and Gil, C. (2019) Imidazole derivatives as promising agents for the treatment of Chagas disease. Antimicrobial Agents and Chemotherapy, 63(4), e02156-18. (doi: 10.1128/AAC.02156-18)

Giordani, F. , Khalaf, A. I., Gillingwater, K., Munday, J. C. , de Koning, H. P. , Suckling, C. J., Barrett, M. P. and Scott, F. J. (2019) Novel minor groove binders cure animal African trypanosomiasis in an in vivo mouse model. Journal of Medicinal Chemistry, 62(6), pp. 3021-3035. (doi: 10.1021/acs.jmedchem.8b01847) (PMID:30763102)

Cerone, M. et al. (2019) Discovery of sustainable drugs for neglected tropical diseases: cashew nut shell liquid (CNSL)-based hybrids target mitochondrial function and ATP production in Trypanosoma brucei. ChemMedChem, 14(6), pp. 621-635. (doi: 10.1002/cmdc.201800790) (PMID:30664325) (PMCID:PMC6686156)

Siheri, W. et al. (2019) Isolation of a novel flavanonol and an alkylresorcinol with highly potent anti-trypanosomal activity from Libyan propolis. Molecules, 24(6), 1041. (doi: 10.3390/molecules24061041) (PMID:30884752)

Hulpia, F., Campagnaro, G. D., Scortichini, M., Van Hecke, K., Maes, L., de Koning, H. P. , Caljon, G. and Van Calenbergh, S. (2019) Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. European Journal of Medicinal Chemistry, 164, pp. 689-705. (doi: 10.1016/j.ejmech.2018.12.050)

Nnadi, C., Ebiloma, G. U., Black, J. A., Nwodo, N., Lemgruber, L. , Schmidt, T. J. and De Koning, H. P. (2019) Potent antitrypanosomal activities of 3-aminosteroids against African trypanosomes: investigation of cellular effects and of cross-resistance with existing drugs. Molecules, 24(2), 268. (doi: 10.3390/molecules24020268) (PMID:30642032)

Hulpia, F., Mabille, D., Campagnaro, G. D., Schumann, G., Maes, L., Roditi, I., Hofer, A., De Koning, H. P. , Caljon, G. and Van Calenbergh, S. (2019) Combining tubercidin and cordycepin scaffolds results in highly active candidates to treat late-stage sleeping sickness. Nature Communications, 10, 5564. (doi: 10.1038/s41467-019-13522-6) (PMID:31804484) (PMCID:PMC6895180)

2018

Campagnaro, G. D., de Freitas Nascimento, J., Girard, R. B.M., Silber, A. M. and de Koning, H. P. (2018) Cloning and characterisation of the Equilibrative Nucleoside Transporter family of Trypanosoma cruzi: ultra-high affinity and selectivity to survive in the intracellular niche. Biochimica et Biophysica Acta: General Subjects, 1862(12), pp. 2750-2763. (doi: 10.1016/j.bbagen.2018.08.015) (PMID:30251664)

Sebastián-Pérez, V., Hendrickx, S., Munday, J. C. , Kalejaiye, T., Martínez, A., Campillo, N. E., de Koning, H. , Caljon, G., Maes, L. and Gil, C. (2018) Cyclic nucleotide specific phosphodiesterases as potential drug targets for anti-Leishmania therapy. Antimicrobial Agents and Chemotherapy, 62(10), e00603-18. (doi: 10.1128/AAC.00603-18) (PMID:30104270)

Meco-Navas, A. et al. (2018) SAR of 4-alkoxybenzoic acid inhibitors of the trypanosome alternative oxidase. ACS Medicinal Chemistry Letters, 9(9), pp. 923-928. (doi: 10.1021/acsmedchemlett.8b00282) (PMID:30258542)

Blaazer, A. R. et al. (2018) Targeting a subpocket in Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) enables the structure-based discovery of selective Inhibitors with trypanocidal activity. Journal of Medicinal Chemistry, 61(9), pp. 3870-3888. (doi: 10.1021/acs.jmedchem.7b01670) (PMID:29672041) (PMCID:PMC5949723)

Ebiloma, G. U. et al. (2018) Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense. European Journal of Medicinal Chemistry, 150, pp. 385-402. (doi: 10.1016/j.ejmech.2018.02.075) (PMID:29544150)

Ebiloma, G. U., Katsoulis, E., Igoli, J. O., Gray, A. I. and De Koning, H. P. (2018) Multi-target mode of action of a clerodane-type diterpenoid from Polyalthia longifolia targeting African trypanosomes. Scientific Reports, 8, 4613. (doi: 10.1038/s41598-018-22908-3) (PMID:29545637) (PMCID:PMC5854603)

Campagnaro, G. D., Alzahrani, K. J., Munday, J. C. and De Koning, H. P. (2018) Trypanosoma brucei bloodstream forms express highly specific and separate transporters for adenine and hypoxanthine; evidence for a new protozoan purine transporter family? Molecular and Biochemical Parasitology, 220, pp. 46-56. (doi: 10.1016/j.molbiopara.2018.01.005) (PMID:29371154)

2017

de Koning, H. P. (2017) Drug resistance in protozoan parasites. Emerging Topics in Life Sciences, 1(6), pp. 627-632. (doi: 10.1042/ETLS20170113)

Millan, C. R., Acosta-Reyes, F. J., Lagartera, L., Ebiloma, G. U., Lemgruber Soares, L. , Nué Martinez, J. J., Saperas, N., Dardonville, C., De Koning, H. P. and Campos, J. L. (2017) Functional and structural analysis of AT-specific minor groove binders that disrupt DNA-protein interactions and cause disintegration of the Trypanosoma brucei kinetoplast. Nucleic Acids Research, 45(14), pp. 8378-8391. (doi: 10.1093/nar/gkx521) (PMID:28637278) (PMCID:PMC5737332)

Alzahrani, K. J.H., Ali, J. A.M., Eze, A. A., Looi, W. L., Tagoe, D. N.A., Creek, D. J., Barrett, M. P. and De Koning, H. P. (2017) Functional and genetic evidence that nucleoside transport is highly conserved in Leishmania species: Implications for pyrimidine-based chemotherapy. International Journal for Parasitology: Drugs and Drug Resistance, 7(2), pp. 206-226. (doi: 10.1016/j.ijpddr.2017.04.003) (PMID:28453984) (PMCID:PMC5407577)

Alzahrani, K. J., Matyugina, E. S., Khandazhinskaya, A. L., Kochetkov, S. N., Seley-Radtke, K. L. and de Koning, H. P. (2017) Evaluation of the antiprotozoan properties of 5'-norcarbocyclic pyrimidine nucleosides. Bioorganic and Medicinal Chemistry Letters, 27(14), pp. 3081-3086. (doi: 10.1016/j.bmcl.2017.05.052) (PMID:28571825)

Ranjbarian, F., Vodnala, M., Alzahrani, K. J.H., Ebiloma, G. U., de Koning, H. P. and Hofer, A. (2017) 9-(2' -Deoxy-2' -fluoro-ß-D-arabinofuranosyl) adenine: a potent antitrypanosomal adenosine analogue that circumvents transport-related drug resistance. Antimicrobial Agents and Chemotherapy, 61(6), e02719-16. (doi: 10.1128/AAC.02719-16) (PMID:28373184) (PMCID:PMC5444181)

Omar, R. et al. (2017) The chemical characterization of Nigerian propolis samples and their activity against Trypanosoma brucei. Scientific Reports, 7, 923. (doi: 10.1038/s41598-017-01038-2) (PMID:28424496) (PMCID:PMC5430459)

Ebiloma, G. U., Igoli, J. O., Katsoulis, E., Donachie, A.-M., Eze, A., Gray, A. I. and de Koning, H. P. (2017) Bioassay-guided isolation of active principles from Nigerian medicinal plants identifies new trypanocides with low toxicity and no cross-resistance to diamidines and arsenicals. Journal of Ethnopharmacology, 202, pp. 256-264. (doi: 10.1016/j.jep.2017.03.028) (PMID:28336470)

Fueyo González, F. J. et al. (2017) Conjugates of 2,4-dihydroxybenzoate and salicylhydroxamate and lipocations display potent antiparasite effects by efficiently targeting the Trypanosoma brucei and Trypanosoma congolense mitochondrion. Journal of Medicinal Chemistry, 60(4), pp. 1509-1522. (doi: 10.1021/acs.jmedchem.6b01740) (PMID:28112515)

2016

Giordani, F. , Morrison, L. J., Rowan, T. G., De Koning, H. P. and Barrett, M. P. (2016) The animal trypanosomiases and their chemotherapy: a review. Parasitology, 143(14), pp. 1862-1889. (doi: 10.1017/S0031182016001268) (PMID:27719692) (PMCID:PMC5142301)

Zoltner, M., Horn, D., de Koning, H. P. and Field, M. C. (2016) Exploiting the Achilles' heel of membrane trafficking in trypanosomes. Current Opinion in Microbiology, 34, pp. 97-103. (doi: 10.1016/j.mib.2016.08.005) (PMID:27614711) (PMCID:PMC5176092)

Eze, A. A., Gould, M. K., Munday, J. C. , Tagoe, D. N.A., Stelmanis, V., Schnaufer, A. and De Koning, H. P. (2016) Reduced mitochondrial membrane potential is a late adaptation of trypanosoma brucei brucei to isometamidium preceded by mutations in the γ subunit of the F1Fo-ATPase. PLoS Neglected Tropical Diseases, 10(8), e0004791. (doi: 10.1371/journal.pntd.0004791) (PMID:27518185) (PMCID:PMC4982688)

Vodnala, M., Ranjbarian, F., Pavlova, A., de Koning, H. P. and Hofer, A. (2016) Trypanosoma brucei methylthioadenosine phosphorylase protects the parasite from the antitrypanosomal effect of deoxyadenosine. Journal of Biological Chemistry, 291(22), pp. 11717-11726. (doi: 10.1074/jbc.M116.715615) (PMID:27036940) (PMCID:PMC4882440)

Dike, V. T., Vihiior, B., Bosha, J. A., Yin, T. M., Ebiloma, G. U., de Koning, H. P. , Igoli, J. O. and Gray, A. I. (2016) Antitrypanosomal activity of a novel taccalonolide from the tubers of Tacca leontopetaloides. Phytochemical Analysis, 27(3-4), pp. 217-221. (doi: 10.1002/pca.2619) (PMID:27313159)

Imamura, H. et al. (2016) Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent. eLife, 5, e12613. (doi: 10.7554/eLife.12613) (PMID:27003289) (PMCID:PMC4811772)

Graf, F. E. et al. (2016) Comparative genomics of drug resistance in Trypanosoma brucei rhodesiense. Cellular and Molecular Life Sciences, 73(17), pp. 3387-3400. (doi: 10.1007/s00018-016-2173-6) (PMID:26973180) (PMCID:PMC4967103)

Omar, R. M.K., Igoli, J., Gray, A. I., Ebiloma, G. U., Clements, C., Fearnley, J., Edrada Ebel, R. A., Zhang, T., De Koning, H. and Watson, D. (2016) Chemical characterisation of Nigerian red propolis and its biological activity against Trypanosoma Brucei. Phytochemical Analysis, 27(2), pp. 107-115. (doi: 10.1002/pca.2605) (PMID:26662866)

Babuadze, G. et al. (2016) Seroepidemiology and molecular diversity of Leishmania donovani complex in Georgia. Parasites and Vectors, 9, 279. (doi: 10.1186/s13071-016-1558-6) (PMID:27177688) (PMCID:PMC4866401)

Siheri, W. et al. (2016) Chemical and antimicrobial profiling of propolis from different regions within Libya. PLoS ONE, 11(5), e0155355. (doi: 10.1371/journal.pone.0155355) (PMID:27195790) (PMCID:PMC4873177)

2015

Alkhaldi, A. A.M., Martinek, J., Panicucci, B., Dardonville, C., Zikova, A. and De Koning, H. (2015) Trypanocidal action of bisphosphonium salts through a mitochondrial target in bloodstream form Trypanosoma brucei. International Journal for Parasitology: Drugs and Drug Resistance, 6(1), pp. 23-34. (doi: 10.1016/j.ijpddr.2015.12.002)

Rodenko, B., Wanner, M., Alkhaldi, A., Ebiloma, G., Barnes, R., Kaiser, M., Brun, R., McCulloch, R. , Koomen, G.-J. and De Koning, H. P. (2015) Targeting the parasite's DNA with methyltriazenyl purine analogs Is a safe, selective, and efficacious antitrypanosomal strategy. Antimicrobial Agents and Chemotherapy, 59(11), pp. 6708-6716. (doi: 10.1128/aac.00596-15) (PMID:26282430) (PMCID:PMC4604408)

Tagoe, D. N. A., Kalejaiye, T. D. and De Koning, H. P. (2015) The ever unfolding story of cAMP signaling in trypanosomatids: vive la difference! Frontiers in Pharmacology, 6, 185. (doi: 10.3389/fphar.2015.00185) (PMID:26441645) (PMCID:PMC4561360)

Graf, F. E., Baker, N., Munday, J. C. , De Koning, H. P. , Horn, D. and Mäser, P. (2015) Chimerization at the AQP2–AQP3 locus is the genetic basis of melarsoprol–pentamidine cross-resistance in clinical Trypanosoma brucei gambiense isolates. International Journal for Parasitology: Drugs and Drug Resistance, 5(2), pp. 65-68. (doi: 10.1016/j.ijpddr.2015.04.002) (PMID:26042196) (PMCID:PMC4443405)

Ríos Martínez, C. H., Nué Martínez, J. J., Ebiloma, G. U., De Koning, H. P. , Alkorta, I. and Dardonville, C. (2015) Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro. European Journal of Medicinal Chemistry, 101, pp. 806-817. (doi: 10.1016/j.ejmech.2015.07.013) (PMID:26231081)

Unciti-Broceta, J. D., Arias, J. L., Maceira, J., Soriano, M., Ortiz-González, M., Hernández-Quero, J., Muñóz-Torres, M., De Koning, H. P. , Magez, S. and Garcia-Salcedo, J. A. (2015) Specific cell targeting therapy bypasses drug resistance mechanisms in African trypanosomiasis. PLoS Pathogens, 11(6), e1004942. (doi: 10.1371/journal.ppat.1004942) (PMID:26110623) (PMCID:PMC4482409)

Munday, J. C. et al. (2015) Functional analysis of drug resistance-associated mutations in the Trypanosoma brucei Adenosine Transporter 1 (TbAT1) and the proposal of a structural model for the protein. Molecular Microbiology, 96(4), pp. 887-900. (doi: 10.1111/mmi.12979) (PMID:25708978) (PMCID:PMC4755147)

Munday, J. C. , Settimo, L. and De Koning, H. P. (2015) Transport proteins determine drug sensitivity and resistance in a protozoan parasite, Trypanosoma brucei. Frontiers in Pharmacology, 6, 32. (doi: 10.3389/fphar.2015.00032) (PMID:24235095) (PMCID:PMC3922157)

Alkhaldi, A.A.M., Creek, D.J., Ibrahim, H., Kim, D.-H., Quashie, N.B., Burgess, K.E., Changtam, C., Barrett, M.P. , Suksamrarn, A. and De Koning, H.P. (2015) Potent Trypanocidal curcumin analogs bearing a monoenone linker motif act on Trypanosoma brucei by forming an adduct with Trypanothione. Molecular Pharmacology, 87(3), pp. 451-464. (doi: 10.1124/mol.114.096016) (PMID:25527638)

Dardonville, C., Alkhaldi, A. A.M. and De Koning, H. P. (2015) SAR studies of diphenyl cationic trypanocides: superior activity of phosphonium over ammonium salts. ACS Medicinal Chemistry Letters, 6(2), pp. 151-155. (doi: 10.1021/ml500408d) (PMID:25699142) (PMCID:PMC4329581)

Ríos Martínez, C. H., Miller, F., Ganeshamoorthy, K., Glacial, F., Kaiser, M., De Koning, H. , Eze, A. A., Lagartera, L., Herraiz, T. and Dardonville, C. (2015) A new nonpolar N-hydroxy imidazoline lead compound with improved activity in a murine model of late-stage Trypanosoma brucei brucei infection is not cross-resistant with diamidines. Antimicrobial Agents and Chemotherapy, 59(2), pp. 890-904. (doi: 10.1128/AAC.03958-14)

Shameer, S. et al. (2015) TrypanoCyc: a community-led biochemical pathways database for Trypanosoma brucei. Nucleic Acids Research, 43(D1), D637-D644. (doi: 10.1093/nar/gku944) (PMID:25300491) (PMCID:PMC4384016)

Natto, M. J., Eze, A. A. and De Koning, H. P. (2015) Protocols for the routine screening of drug sensitivity in the human parasite Trichomonas vaginalis. In: Hempel, J. E., Williams, C. H. and Hong, C. C. (eds.) Chemical Biology. Series: Methods in molecular biology (1263). Humana Press: New York, pp. 103-110. ISBN 9781493922680 (doi: 10.1007/978-1-4939-2269-7_8)

Quashie, N. B., Ranford-Cartwright, L. C. and de Koning, H. P. (2015) Towards antimalarial drug discovery: purine transporters in Plasmodium falciparum as a possible drug target. In: Adjei, G. O. and Ofori-Adjei, D. (eds.) Towards Safe and Effective Treatment of Disease in Ghana: Contributions From Clinical Pharmacology. Series: University of Ghana readers; clinical sciences series (13). Digibooks Ghana Ltd: Tema, Ghama, pp. 109-135. ISBN 9789988219093

2014

Acosta-Reyes, F. J., Dardonville, C., De Koning, H. P. , Natto, M., Subirana, J. A. and Campos, J. L. (2014) In and out of the minor groove: interaction of an AT-rich DNA with the drug CD27. Acta Crystallographica. Section D: Biological Crystallography, 70(6), pp. 1614-1621. (doi: 10.1107/S139900471400697X)

Lüscher, A., Lamprea-Burgunder, E., Graf, F. E., De Koning, H. and Mäser, P. (2014) Trypanosoma brucei adenine-phosphoribosyltransferases mediate adenine salvage and aminopurinol susceptibility but not adenine toxicity. International Journal for Parasitology: Drugs and Drug Resistance, 4(1), pp. 55-63. (doi: 10.1016/j.ijpddr.2013.12.001)

Munday, J. C. et al. (2014) Trypanosoma brucei aquaglyceroporin 2 is a high-affinity transporter for pentamidine and melaminophenyl arsenic drugs and the main genetic determinant of resistance to these drugs. Journal of Antimicrobial Chemotherapy, 69(3), pp. 651-663. (doi: 10.1093/jac/dkt442) (PMID:24235095) (PMCID:PMC3922157)

Babuadze, G. et al. (2014) Epidemiology of Visceral Leishmaniasis in Georgia. PLoS Neglected Tropical Diseases, 8(3), e2725. (doi: 10.1371/journal.pntd.0002725)

Garcia-Salcedo, J. A., Munday, J. C. , Unciti-Broceta, J. D. and De Koning, H. P. (2014) Progress towards new treatments for human African trypanosomiasis. In: Magez, S. and Radwanska, M. (eds.) Trypanosomes and Trypanosomiasis. Springer, pp. 217-238. ISBN 9783709115558 (doi: 10.1007/978-3-7091-1556-5_9)

Zimmermann, S. C., O'Neill, E., Ebiloma, G. U., Wallace, L. J.M., De Koning, H. P. and Seley-Radtke, K. L. (2014) Design and synthesis of a series of truncated neplanocin fleximers. Molecules, 19(12), pp. 21200-21214. (doi: 10.3390/molecules191221200)

2013

Munday, J.C. , Rojas López, K.E., Eze, A.A., Delespaux, V., Van Den Abbeele, J., Rowan, T., Barrett, M.P. , Morrison, L.J. and De Koning, H.P. (2013) Functional expression of TcoAT1 reveals it to be a P1-type nucleoside transporter with no capacity for diminazene uptake. International Journal for Parasitology: Drugs and Drug Resistance, 3, pp. 69-76. (doi: 10.1016/j.ijpddr.2013.01.004)

Vodnala, S.K. et al. (2013) Structure–activity relationships of synthetic cordycepin analogues as experimental therapeutics for African trypanosomiasis. Journal of Medicinal Chemistry, 56(24), pp. 9861-9873. (doi: 10.1021/jm401530a)

Graf, F. E., Wenzler, T., Ludin, P., Kaiser, M., Brun, R., Pyana, P. P., Buscher, P., De Koning, H. P. , Horn, D. and Maser, P. (2013) Aquaporin 2 mutations in Trypanosoma brucei gambiense field isolates correlate with decreased susceptibility to pentamidine and melarsoprol. PLoS Neglected Tropical Diseases, 7(10), e2475. (doi: 10.1371/journal.pntd.0002475)

Gould, M.K., Bachmaier, S., Ali, J.A.M., Alsford, S., Tagoe, D.N.A., Munday, J.C. , Schnaufer, A.C., Horn, D., Boshart, M. and De Koning, H. (2013) Cyclic AMP effectors in African trypanosomes revealed by genome-scale RNA interference library screening for resistance to the phosphodiesterase inhibitor CpdA. Antimicrobial Agents and Chemotherapy, 57(10), pp. 4882-4893. (doi: 10.1128/AAC.00508-13)

Baker, N., De Koning, H.P. , Mäser, P. and Horn, D. (2013) Drug resistance in African trypanosomiasis: the melarsoprol and pentamidine story. Trends in Parasitology, 29(3), pp. 110-118. (doi: 10.1016/j.pt.2012.12.005)

Ali, J.A.M., Creek, D.J., Burgess, K., Allison, H.C., Field, M.C., Maser, P. and De Koning, H.P. (2013) Pyrimidine salvage in trypanosoma brucei bloodstream forms and the trypanocidal action of halogenated pyrimidines. Molecular Pharmacology, 83(2), pp. 439-453. (doi: 10.1124/mol.112.082321) (PMID:23188714)

Ali, J. A.., Tagoe, D. N.A., Munday, J. C. , Donachie, A., Morrison, L. J. and De Koning, H. P. (2013) Pyrimidine biosynthesis is not an essential function for trypanosoma brucei bloodstream forms. PLoS ONE, 8(3), e58034. (doi: 10.1371/journal.pone.0058034) (PMID:23505454) (PMCID:PMC3591441)

Delespaux, V. and De Koning, H. (2013) Transporters in anti-parasitic drug development and resistance. In: Jäger, T., Koch, O. and Flohé, L. (eds.) Trypanosomatid Diseases: Molecular Routes to Drug Discovery. Series: Drug discovery in infectious diseases (4). John Wiley and Sons Ltd.: Weinheim, pp. 335-349. ISBN 9783527332557 (doi: 10.1002/9783527670383.ch18)

Rodenko, B. and De Koning, H. (2013) Rational selection of anti-microbial drug targets: unique or conserved? In: Jäger, T., Koch, O. and Flohé, L. (eds.) Trypanosomatid Diseases: Molecular Routes to Drug Discovery. Series: Drug discovery in infectious diseases (4). Wiley-Blackwell: Weinheim, pp. 279-296. ISBN 9783527332557 (doi: 10.1002/9783527670383.ch15)

2012

Baker, N., Glover, L., Munday, J. C. , Aguinaga Andres, D., Barrett, M. P. , De Koning, H. P. and Horn, D. (2012) Aquaglyceroporin 2 controls susceptibility to melarsoprol and pentamidine in African trypanosomes. Proceedings of the National Academy of Sciences of the United States of America, 109(27), pp. 10996-11001. (doi: 10.1073/pnas.1202885109)

De Koning, H.P. , Gould, M.K., Sterk, G.J., Tenor, H., Kunz, S., Luginbuehl, E. and Seebeck, T. (2012) Pharmacological validation of Trypanosoma brucei phosphodiesterases as novel drug targets. Journal of Infectious Diseases, 206(2), pp. 229-237. (doi: 10.1093/infdis/jir857)

Natto, M.J., Savioli, F., Quashie, N.B., Dardonville, C., Rodenko, B. and De Koning, H.P. (2012) Validation of novel fluorescence assays for the routine screening of drug susceptibilities of Trichomonas vaginalis. Journal of Antimicrobial Chemotherapy, 67(4), pp. 933-943. (doi: 10.1093/jac/dkr572)

Taladriz, A. et al. (2012) Synthesis and structure–activity analysis of new phosphonium salts with potent activity against African Trypanosomes. Journal of Medicinal Chemistry, 55(6), pp. 2606-2622. (doi: 10.1021/jm2014259)

2011

Teka, I. A. et al. (2011) The diamidine diminazene aceturate is a substrate for the high-affinity pentamidine transporter: implications for the development of high resistance levels in trypanosomes. Molecular Pharmacology, 80(1), pp. 110-116. (doi: 10.1124/mol.111.071555)

Ibrahim, H.M.S., Al-Salabi, M.I., El Sabbagh, N., Quashie, N.B., Alkhaldi, A.A.M., Escale, R., Smith, T.K., Vial, H.J. and De Koning, H.P. (2011) Symmetrical choline-derived dications display strong anti-kinetoplastid activity. Journal of Antimicrobial Chemotherapy, 66(1), pp. 111-125. (doi: 10.1093/jac/dkq401)

Gould, M.K. and De Koning, H.P. (2011) Cyclic-nucleotide signalling in protozoa. FEMS Microbiology Reviews, 31(3), pp. 515-541. (doi: 10.1111/j.1574-6976.2010.00262.x)

Rodenko, B., Al-Salabi, M.I., Teka, I.A., Ho, W., El-Sabbagh, N., Ali, J.A.M., Ibrahim, H.M.S., Wanner, M.J., Koomen, G.-J. and De Koning, H.P. (2011) Synthesis of marine-derived 3-alkylpyridinium alkaloids with potent antiprotozoal activity. ACS Medicinal Chemistry Letters, 2(12), pp. 901-906. (doi: 10.1021/ml200160k)

Shakur, Y., De Koning, H.P. , Ke, H., Kambayashi, J. and Seebeck, T. (2011) Therapeutic potential of phosphodiesterase inhibitors in parasitic diseases. Handbook of Experimental Pharmacology, 204, pp. 487-510. (doi: 10.1007/978-3-642-17969-3_20)

Ward, C.P., Wong, P.E., Burchmore, R.J.S. , De Koning, H.P. and Barrett, M.P. (2011) Trypanocidal furamidine analogues: influence of pyridine nitrogens on trypanocidal activity, transport kinetics, and resistance patterns. Antimicrobial Agents and Chemotherapy, 55(5), pp. 2352-2361. (doi: 10.1128/AAC.01551-10)

2010

Paine, M.F. et al. (2010) Diamidines for human African trypanosomiasis. Current Opinion in Investigational Drugs, 11(8), pp. 876-883.

Berg, M. et al. (2010) Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. Antimicrobial Agents and Chemotherapy, 54(5), pp. 1900-1908. (doi: 10.1128/AAC.01787-09)

Changtam, C., de Koning, H.P. , Ibrahim, H., Sajid, M.S., Gould, M.K. and Suksamrarn, A. (2010) Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species. European Journal of Medicinal Chemistry, 45(3), pp. 941-956. (doi: 10.1016/j.ejmech.2009.11.035)

Stewart, M.L. et al. (2010) Multiple genetic mechanisms lead to loss of functional TbAT1 expression in drug-resistant trypanosomes. Eukaryotic Cell, 9(2), pp. 336-343. (doi: 10.1128/EC.00200-09) (PMID:19966032) (PMCID:PMC2823006)

Altink, R., van Arkel, B., van der Baan, J.L., Balt, S., De Bolster, M.W.G., van Delft, R.J., Klumpp, G.W., De Koning, H. and van den Winkel, Y. (2010) A new model for coenzyme B12 based on a Costa-type ligand. Recueil des Travaux Chimiques des Pays-Bas, 113(6), pp. 329-333. (doi: 10.1002/recl.19941130604)

Quashie, N.B., Ranford-Cartwright, L.C. and De Koning, H.P. (2010) Uptake of purines in Plasmodium falciparum-infected human erythrocytes is mostly mediated by the human Equilibrative Nucleoside Transporter and the human Facilitative Nucleobase Transporter. Malaria Journal, 9(36), (doi: 10.1186/1475-2875-9-36)

Ward, C. P., Burgess, K. E.V., Burchmore, R.J.S. , Barrett, M.P. and De Koning, H.P. (2010) A fluorescence-based assay for the uptake of CPD0801 (DB829) by African trypanosomes. Molecular and Biochemical Parasitology, 174(2), pp. 145-149. (doi: 10.1016/j.molbiopara.2010.07.002)

2009

Kazibwe, A.J.N., Nerima, B., De Koning, H.P. , Mäser, P., Barrett, M.P. and Matovu, E. (2009) Genotypic status of the TbAT1/P2 adenosine transporter of Trypanosoma brucei gambiense isolates from northwestern Uganda following melarsoprol withdrawal. PLoS Neglected Tropical Diseases, 3(9), e523. (doi: 10.1371/journal.pntd.0000523)

Sanderson, L., Dogruel, M., Rodgers, J. , De Koning, H.P. and Thomas, S.A. (2009) Pentamidine Movement across the Murine Blood-Brain and Blood-Cerebrospinal Fluid Barriers: Effect of Trypanosome Infection, Combination Therapy, P-Glycoprotein, and Multidrug Resistance-Associated Protein. Journal of Pharmacology and Experimental Therapeutics, 329(3), pp. 967-977. (doi: 10.1124/jpet.108.149872)

Collar, C.J., Al Salabi, M.I., Stewart, M.L., Barrett, M.P. , Wilson, W.D. and de Koning, H.P. (2009) Predictive computational models of substrate binding by a nucleoside transporter. Journal of Biological Chemistry, 284(49), pp. 34028-34035. (doi: 10.1074/jbc.M109.049726)

2008

Gould, M.K., Vu, X.L., Seebeck, T. and De Koning, H.P. (2008) Propidium iodide-based methods for monitoring drug action in the kinetoplastidae: Comparison with the Alamar Blue assay. Analytical Biochemistry, 382(2), pp. 87-93. (doi: 10.1016/j.ab.2008.07.036)

Quashie, N.B., Dorin-Semblat, D., Bray, P.G., Biagini, G.A., Doerig, C., Ranford-Cartwright, L.C. and De Koning, H.P. (2008) A comprehensive model of purine uptake by the malaria parasite Plasmodium falciparum: identification of four purine transport activities in intraerythrocytic parasites. Biochemical Journal, 411(2), pp. 287-295. (doi: 10.1042/BJ20071460)

De Koning, H.P. (2008) Ever-increasing complexities of diamidine and arsenical crossresistance in African trypanosomes. Trends in Parasitology, 24(8), pp. 345-349. (doi: 10.1016/j.pt.2008.04.006)

Papageorgiou, I., De Koning, H.P., Soteriadou, K. and Diallinas, G. (2008) Kinetic and mutational analysis of the Trypanosoma brucei NBT1 nucleobase transporter expressed in Saccharomyces cerevisiae reveals structural similarities between ENT and MFS transporters. International Journal for Parasitology, 38(6), pp. 641-653. (doi: 10.1016/j.ijpara.2007.10.005)

2007

Rodenko, B., van der Burg, A. M., Wanner, M. J., Kaiser, M., Brun, R., Gould, M., de Koning, H. P. and Koomen, G.-J. (2007) 2,N⁶-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities. Antimicrobial Agents and Chemotherapy, 51(11), pp. 3796-3802. (doi: 10.1128/AAC.00425-07) (PMID:17698622) (PMCID:PMC2151466)

De Koning, H. P. (2007) Pyrimidine transporters of trypanosomes: a class apart? Trends in Parasitology, 23(5), p. 190. (doi: 10.1016/j.pt.2007.03.004)

Bridges, D. J., Gould, M. K., Nerima, B., Maser, P., Burchmore, R. J. S. and de Koning, H. P. (2007) Loss of the high-affinity pentamidine transporter is responsible for high levels of cross-resistance between arsenical and diamidine drugs in African trypanosomes. Molecular Pharmacology, 71, pp. 1098-1108. (doi: 10.1124/mol.106.031351)

Al-Salabi, M., Wallace, L., Luscher, A., Maser, P., Candlish, D., Rodenko, B., Gould, M., Jabeen, I., Ajith, S. and de Koning, H. (2007) Molecular interactions underlying the unusually high adenosine affinity of a novel Trypanosoma brucei nucleoside transporter. Molecular Pharmacology, 71, pp. 921-929. (doi: 10.1124/mol.106.031559)

Delespaux, V. and de Koning, H. (2007) Drugs and drug resistance in African trypanosomiasis. Drug Resistance Updates, 10, pp. 30-50. (doi: 10.1016/j.drup.2007.02.004)

Luscher, A., de Koning, H. and Maser, P. (2007) Chemotherapeutic strategies against Trypanosoma brucei: Drug targets vs. drug targeting. Current Pharmaceutical Design, 13, pp. 555-567.

2006

Quashie, N. B., de Koning, H. P. and Ranford-Cartwright, L. C. (2006) An improved and highly sensitive microfluorimetric method for assessing susceptibility of Plasmodium falciparum to antimalarial drugs in vitro. Malaria Journal, 5, 95. (doi: 10.1186/1475-2875-5-95) (PMID:17076900) (PMCID:PMC1657019)

Anene, B.M., Ezeokonkwo, R.C., Mmesirionye, T.I., Tettey, J.N.A., Brock, J.M., Barrett, M.P. and De Koning, H.P. (2006) A diminazene-resistant strain of Trypanosoma brucei brucei isolated from a dog is cross-resistant to pentamidine in experimentally infected albino rats. Parasitology, 132(1), pp. 127-133. (doi: 10.1017/S0031182005008760)

Gudin, S., Quashie, N., Candlish, D., Al-Salabi, M., Jarvis, S., Ranford-Cartwright, L. and de Koning, H. (2006) Trypanosoma brucei: A survey of pyrimidine transport activities. Experimental Parasitology, 114, pp. 118-125. (doi: 10.1016/j.expara.2006.02.018)

Stoffel, S., Rodenko, B., Schweingruber, A., Maser, P., de Koning, H. and Schweingruber, M. (2006) Biosynthesis and uptake of thiamine (vitamin B-1) in bloodstream form Trypanosoma brucei brucei and interference of the vitamin with melarsen oxide activity. International Journal for Parasitology, 36, pp. 229-236. (doi: 10.1016/j.ijpara.2005.10.003)

2005

De Koning, H. P. , Bridges, D. J. and Burchmore, R. J. S. (2005) Purine and pyrimidine transport in pathogenic protozoa: From biology to therapy. FEMS Microbiology Reviews, 29(5), pp. 987-1020. (doi: 10.1016/j.femsre.2005.03.004)

Geiser, F., Lüscher, A., De Koning, H.P. , Seebeck, T. and Mäser, P. (2005) Molecular pharmacology of adenosine transport in trypanosoma brucei: P1/P2 revisited. Molecular Pharmacology, 68(3), pp. 589-595. (doi: 10.1124/mol.104.010298)

Natto, M.J., Wallace, L.J.M., Candlish, D., Al-Salabi, M.I., Coutts, S.E. and de Koning, H.P. (2005) Trypanosoma brucei: expression of multiple purine transporters prevents the development of allopurinol resistance. Experimental Parasitology, 109(2), pp. 80-86. (doi: 10.1016/j.exppara.2004.11.004)

Al-Salabi, M. and de Koning, H. (2005) Purine nucleobase transport in amastigotes of Leishmania mexicana: Involvement in allopurinol uptake. Antimicrobial Agents and Chemotherapy, 49, pp. 3682-3689. (doi: 10.1128/AAC.49.9.3682-3689.2005)

Papageorgiou, I., Yakob, L., Al Salabi, M., Diallinas, G., Soteriadou, K. and De Koning, H. (2005) Identification of the first pyrimidine nucleobase transporter in Leishmania: similarities with the Trypanosoma brucei U1 transporter and antileishmanial activity of uracil analogues. Parasitology, 130, pp. 275-283. (doi: 10.1017/S0031182004006626)

Stewart, M., Krishna, S., Burchmore, R. , Brun, R., de Koning, H. , Boykin, D., Tidwell, R., Hall, J. and Barrett, M. (2005) Detection of arsenical drug resistance in Trypanosoma brucei with a simple fluorescence test. Lancet, 366, pp. 486-487. (doi: 10.1016/S0140-6736(05)66793-1)

2004

Biagini, G., Pasini, E., Hughes, R., De Koning, H. , Vial, H., ONeill, P., Ward, S. and Bray, P. (2004) Characterization of the choline carrier of Plasmodium falciparum: a route for the selective delivery of novel antimalarial chugs. Blood, 104, pp. 3372-3377.

de Koning, H. , Anderson, L., Stewart, M., Burchmore, R. , Wallace, L. and Barrett, M. (2004) The trypanocide diminazene aceturate is accumulated predominantly through the TbAT1 purine transporter: additional insights on diamidine resistance in African trypanosomes. Antimicrobial Agents and Chemotherapy, 48, pp. 1515-1519. (doi: 10.1128/AAC.48.5.1515-1519.2004)

Wallace, L., Candlish, D., Hagos, A., Seley, K. and de Koning, H. (2004) Selective transport of a new class of purine antimetabolites by the protozoan parasite Trypanosoma brucei. Nucleosides Nucleotides and Nucleic Acids, 23, pp. 1441-1444. (doi: 10.1081/NCN-200027660)

2003

De Koning, H. , Al-Salabi, M., Cohen, A., Coombs, G. and Wastling, J. (2003) Identification and characterisation of high affinity nucleoside and nucleobase transporters in Toxoplasma gondii. International Journal for Parasitology, 33(8), pp. 821-831. (doi: 10.1016/S0020-7519(03)00091-2)

Al-Salabi, M., Wallace, L. and De Koning, H. (2003) A Leishmania major nucleobase transporter responsible for allopurinol uptake is a functional homolog of the Trypanosoma brucei H2 transporter. Molecular Pharmacology, 63, pp. 814-820.

Bray, P., Barrett, M. , Ward, S. and de Koning, H. (2003) Pentamidine uptake and resistance in pathogenic protozoa: past, present and future. Trends in Parasitology, 19(5), pp. 232-239. (doi: 10.1016/S1471-4922(03)00069-2)

Burchmore, R. , Wallace, L., Candlish, D., Al-Salabi, M., Beal, P., Barrett, M. , Baldwin, S. and de Koning, H. (2003) Cloning, heterologous expression, and in situ characterization of the first high affinity nucleobase transporter from a protozoan. Journal of Biological Chemistry, 278(26), pp. 23502-23507. (doi: 10.1074/jbc.M301252200)

Matovu, E. et al. (2003) Mechanisms of arsenical and diamidine uptake and resistance in Trypanosoma brucei. Eukaryotic Cell, 2(5), pp. 1003-1008. (doi: 10.1128/EC.2.5.1003-1008.2003)

2002

Wallace, L., Candlish, D. and De Koning, H. (2002) Different substrate recognition motifs of human and trypanosome nucleobase transporters - Selective uptake of purine antimetabolites. Journal of Biological Chemistry, 277, pp. 26149-26156. (doi: 10.1074/jbc.M202835200)

2001

Stead, A.M.W., Bray, P.G., Edwards, I.G., De Koning, H.P. , Elford, B.C., Stocks, P.A. and Ward, S. (2001) Diamidine compounds: Selective uptake and targeting in Plasmodium falciparum. Molecular Pharmacology, 59(5), pp. 1298-1306.

De Koning, H. (2001) Transporters in African trypanosomes: role in drug action and resistance. International Journal for Parasitology, 31(5-6), pp. 511-521. (doi: 10.1016/S0020-7519(01)00167-9)

de Koning, H. (2001) Uptake of pentamidine in Trypanosoma brucei brucei is mediated by three distinct transporters: Implications for cross-resistance with arsenicals. Molecular Pharmacology, 59, pp. 586-592.

de Koning, H. and Jarvis, S. (2001) Uptake of pentamidine in Trypanosoma brucei brucei is mediated by the P2 adenosine transporter and at least one novel, unrelated transporter. Acta Tropica, 80, pp. 245-250.

2000

De Koning, H. and Diallinas, G. (2000) Nucleobase transporters: review. Molecular Membrane Biology, 17(2), pp. 75-94. (doi: 10.1080/09687680050117101)

De Koning, H.P. , MacLeod, A. , Barrett, M.P. , Cover, B. and Jarvis, S.M. (2000) Further evidence for a link between melarsoprol resistance and P2 transporter function in African trypanosomes. Molecular and Biochemical Parasitology, 106(1), pp. 181-185. (doi: 10.1016/S0166-6851(99)00206-6)

De Koning, H.P. , Watson, C.J., Sutcliffe, L. and Jarvis, S.M. (2000) Differential regulation of nucleoside and nucleobase transporters in Crithidia fasciculata and Trypanosoma brucei brucei. Molecular and Biochemical Parasitology, 106(1), pp. 93-107. (doi: 10.1016/S0166-6851(99)00203-0)

1999

Carter, N.S., Barrett, M.P. and De Koning, H.P. (1999) A drug resistance determinant in trypanosoma brucei. Trends in Microbiology, 7(12), pp. 469-471. (doi: 10.1016/S0966-842X(99)01643-1)

De Koning, H.P. and Jarvis, S.M. (1999) Adenosine transporters in bloodstream forms of trypanosoma brucei brucei: substrate recognition motifs and affinity for trypanocidal drugs. Molecular Pharmacology, 56(6), pp. 1162-1170.

1998

De Koning, H.P. and Jarvis, S.M. (1998) A highly selective, high-affinity transporter for uracil in trypanosoma brucei brucei: evidence for proton-dependent transport. Biochemistry and Cell Biology, 76(5), pp. 853-858. (doi: 10.1139/o98-086)

Jenkd, B., Buzzi, M., Dotman, C., De Koning, H. , Scheenen, W., Lisete, J., Leenders, H., Cruijsen, P. and Roubos, E. (1998) The significance of multiple inhibitory mechanisms converging on the melanotrope cell of Xenopus laevisa. Annals of the New York Academy of Sciences, 839, pp. 229-234. (doi: 10.1111/j.1749-6632.1998.tb10765.x)

De Koning, H.P. , Watson, C.J. and Jarvis, S.M. (1998) Characterization of a nucleoside/proton symporter in procyclic trypanosoma brucei brucei. Journal of Biological Chemistry, 273(16), pp. 9486-9494. (doi: 10.1074/jbc.273.16.9486)

1997

De Koning, H.P. and Jarvis, S.M. (1997) Purine nucleobase transport in bloodstream forms of trypanosoma brucei brucei is mediated by two novel transporters. Molecular and Biochemical Parasitology, 89(2), pp. 245-258. (doi: 10.1016/S0166-6851(97)00129-1)

De Koning, H.P. and Jarvis, S.M. (1997) Hypoxanthine iptake through a purine-selective nucleobase transporter in trypano soma brucei brucei procyclic cells is driven by protonmotive force. European Journal of Biochemistry, 247(3), pp. 1102-1110. (doi: 10.1111/j.1432-1033.1997.01102.x)

De Koning, H. P. and Jarvis, S. M. (1997) Purine nucleobase transport in bloodstream forms of Trypanosoma brucei brucei. Biochemical Society Transactions, 25, 476S. (doi: 10.1042/bst025476s)

1995

de Koning, H. P. and Jarvis, S. M. (1995) Purine-selective nucleobase transport in Trypanosoma brucei brucei procyclics. Journal of Physiology, 489(suppl), pp. 126-127. (doi: 10.1113/jphysiol.1995.sp021115)

1994

Scheenen, W. J.J.M., De Koning, H. P. , Jenks, B. G., Vaudry, H. and Roubos, E. W. (1994) The secretion of a-MSH from Xenopus melanotropes involves calcium influx through m-conotoxin-sensitive voltage-operated calcium channels. Journal of Neuroendocrinology, 6(4), pp. 457-464. (doi: 10.1111/j.1365-2826.1994.tb00607.x)

1993

De Koning, H.P. , Jenks, B.G. and Roubos, E.W. (1993) Analysis of gamma-aminobutyric acidB receptor function in the in vitro and in vivo regulation of alpha-melanotropin-stimulating hormone secretion from melanotrope cells of Xenopus laevis. Endocrinology, 132(2), pp. 674-681. (doi: 10.1210/endo.132.2.8381070)

Jenks, B.G., De Koning, H.P. , Cruisjen, P.M.J.M., Mauger, C.M.A., Roubos, E.W., Tonon, M.C., Desrues, L. and Vaudry, H. (1993) Analysis of inositol phosphate metabolism in melanotrope cells of Xenopus laevis in relation to background adaptation. Annals of the New York Academy of Sciences, 680, pp. 188-198. (doi: 10.1111/j.1749-6632.1993.tb19684.x)

Jenks, B. G., De Koning, H. P. , Valentijn, K. and Roubos, E. W. (1993) Dual action of GABA_A receptors on the secretory process of melanotrophs of Xenopus laevis. Neuroendocrinology, 58(1), pp. 80-85. (doi: 10.1159/000126516)

Leenders, H.J., De Koning, H.P. , Ponten, S.P., Jenks, B.G. and Roubos, E.W. (1993) Differential effects of coexisting dopamine, GABA and NPY on α-MSH secretion from melanotrope cells of Xenopus laevis. Life Sciences, 52(24), pp. 1969-1975. (doi: 10.1016/0024-3205(93)90638-J)

1992

De Koning, H. P./ , Jenks, B. G., Scheenen, W. J.J.M., Balm, P. H.M. and Roubos, E. W. (1992) Analysis of autofeedback mechanisms in the secretion of pro-opiomelanocortin-derived peptides by melanotrope cells of Xenopus laevis. General and Comparative Endocrinology, 87(3), pp. 394-401. (doi: 10.1016/0016-6480(92)90046-M)

De Koning, H. P. (1992) Receptors and Signal Transduction in the Pars Intermedia of Xenopus Laevis. Krips Repro. ISBN 9789090054001

De Koning, H. P. , Jenks, B. G., Huchede, B. and Roubos, E. W. (1992) Dynamics of cyclic-AMP efflux in relation to α-MSH secretion from melanotrope cells of Xenopus laevis. Life Sciences, 51(21), pp. 1667-1673. (doi: 10.1016/0024-3205(92)90311-C)

1991

De Koning, H. P. , Jenks, B. G., Scheenen, W. J.J.M., de Rijk, E. P.C.T., Cans, R. T.J.M. and Roubos, E. W. (1991) Indirect action of elevated potassium and neuropeptide y on αMSH secretion from the pars intermedia of Xenopus laevi: a biochemical and morphological study. Neuroendocrinology, 54(1), pp. 68-76. (doi: 10.1159/000125853)

Jenks, B.G., van Zoest, I.D., De Koning, H.P. , Leenders, H.J. and Roubos, E.W. (1991) The CRF-related peptide sauvagine stimulates and the GABA_B receptor agonist baclofen inhibits cyclic-AMP production in melanotrope cells of Xenopus laevis. Life Sciences, 48(17), pp. 1633-1637. (doi: 10.1016/0024-3205(91)90123-S)

1988

van Arkel, B., van der Baan, J.L., Balt, S., de Bolster, M. W.G., van Delft, R.J., Klumpp, G.W., De Koning, H. and van den Winkel, Y. (1988) A new model for coenzyme B₁₂. Recueil des Travaux Chimiques des Pays-Bas, 107(1), pp. 23-24. (doi: 10.1002/recl.19881070106)

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