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The diamidine diminazene aceturate is a substrate for the high-affinity pentamidine transporter: implications for the development of high resistance levels in trypanosomes.
Teka IA, Kazibwe AJ, El-Sabbagh N, Al-Salabi MI, Ward CP, Eze AA, Munday JC, Mäser P, Matovu E, Barrett MP, de Koning HP. Teka IA, et al. Among authors: de koning hp. Mol Pharmacol. 2011 Jul;80(1):110-6. doi: 10.1124/mol.111.071555. Epub 2011 Mar 24. Mol Pharmacol. 2011. PMID: 21436312 Free PMC article.
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.
Munday JC, Eze AA, Baker N, Glover L, Clucas C, Aguinaga Andrés D, Natto MJ, Teka IA, McDonald J, Lee RS, Graf FE, Ludin P, Burchmore RJ, Turner CM, Tait A, MacLeod A, Mäser P, Barrett MP, Horn D, De Koning HP. Munday JC, et al. Among authors: de koning hp. J Antimicrob Chemother. 2014 Mar;69(3):651-63. doi: 10.1093/jac/dkt442. Epub 2013 Nov 13. J Antimicrob Chemother. 2014. PMID: 24235095 Free PMC article.
Functional expression of TcoAT1 reveals it to be a P1-type nucleoside transporter with no capacity for diminazene uptake.
Munday JC, Rojas López KE, Eze AA, Delespaux V, Van Den Abbeele J, Rowan T, Barrett MP, Morrison LJ, de Koning HP. Munday JC, et al. Among authors: de koning hp. Int J Parasitol Drugs Drug Resist. 2013 Feb 10;3:69-76. doi: 10.1016/j.ijpddr.2013.01.004. eCollection 2013 Dec. Int J Parasitol Drugs Drug Resist. 2013. PMID: 24533295 Free PMC article.
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.
Ríos Martínez CH, Miller F, Ganeshamoorthy K, Glacial F, Kaiser M, de Koning HP, Eze AA, Lagartera L, Herraiz T, Dardonville C. Ríos Martínez CH, et al. Among authors: de koning hp. Antimicrob Agents Chemother. 2015 Feb;59(2):890-904. doi: 10.1128/AAC.03958-14. Epub 2014 Nov 24. Antimicrob Agents Chemother. 2015. PMID: 25421467 Free PMC article.
Design and synthesis of a series of truncated neplanocin fleximers.
Zimmermann SC, O'Neill E, Ebiloma GU, Wallace LJ, De Koning HP, Seley-Radtke KL. Zimmermann SC, et al. Among authors: de koning hp. Molecules. 2014 Dec 16;19(12):21200-14. doi: 10.3390/molecules191221200. Molecules. 2014. PMID: 25521119 Free PMC article.
186 results