Short technical reportA fluorescence-based assay for the uptake of CPD0801 (DB829) by African trypanosomes
Graphical abstract
. A fluorescence based method for quantifying the uptake of CPD0801 (DB829), a drug candidate against second stage HAT, by African trypanosomes.
Research highlights
▶ CPD0801, a novel diamidine, has potent trypanocidal activity. ▶ Like other diamidines it is carried into trypanosomes principally via the P2 aminopurine transporter. ▶ Here we report a simple fluorescence based method to quantitate uptake.
Section snippets
Acknowledgements
We thank Prof. David Boykin for providing CPD0801, Pui Ee Wong and Mohammed Al-Salabi for assistance with animal handling, and Darren Creek with help in analysing the HPLC-UV and HPLC–MSMS data. This work was supported by the Bill and Melinda Gates Foundation through the Consortium of Parasitic Drug Development (CPDD).
References (20)
- et al.
Effectiveness of melarsoprol and eflornithine as first-line regimens for gambiense sleeping sickness in nine Médecins Sans Frontières programmes
Trans R Soc Trop Med Hyg
(2009) - et al.
Pentamidine uptake and resistance in pathogenic protozoa: past, present and future
Trends Parasitol
(2003) - et al.
Genetic variants of the TbAT1 adenosine transporter from African trypanosomes in relapse infections following melarsoprol therapy
Mol Biochem Parasitol
(2001) - et al.
Uptake of pentamidine in Trypanosoma brucei brucei is mediated by the P2 adenosine transporter and at least one novel, unrelated transporter
Acta Trop
(2001) - et al.
Detection of arsenical drug resistance in Trypanosoma brucei with a simple fluorescence test
Lancet
(2005) - et al.
Comparison of isometamidium chloride and homidium bromide as prophylactic drugs for trypanosomiasis in cattle at Nguruman, Kenya
Acta Trop
(1995) - et al.
On the DNA content and ploidy of trypanosomes
Mol Biochem Parasitol
(1982) - et al.
Differentiation of Trypanosoma brucei bloodstream trypomastigotes from long slender to short stumpy-like forms in axenic culture
Mol Biochem Parasitol
(1990) - et al.
Differential regulation of nucleoside and nucleobase transporters in Crithidia fasciculata and Trypanosoma brucei brucei
Mol Biochem Parasitol
(2000) - et al.
Purine transporters of protozoa: from biology to therapy
FEMS Microbiol Rev
(2005)
There are more references available in the full text version of this article.
Cited by (9)
Synthesis of new thienylnicotinamidines: Proapoptotic profile and cell cycle arrest of HepG2 cells
2022, Archiv der PharmazieA review of cationic arylfurans and their isosteres: Synthesis and biological importance
2019, Current Organic ChemistryIndependence from kinetoplast DNA maintenance and expression is associated with multidrug resistance in trypanosoma brucei in vitro
2014, Antimicrobial Agents and ChemotherapyHydrophilic interaction chromatography in drug analysis
2012, Central European Journal of Chemistry
Copyright © 2010 Elsevier B.V. All rights reserved.