Dianne Damper, Curtis L. Patton
Feb 1, 1976
Citations
0
Influential Citations
60
Citations
Journal
Biochemical pharmacology
Abstract
Abstract Pentamidine, an aromatic diamidine used in the treatment and control of African trypanosomiases, is rapidly absorbed by Trypanosoma brucei and is lethal to the parasite both in vitro and in vivo . The pentamidine transport system in T. brucei exhibits saturation kinetics and shows specificity for the aromatic amidine moiety of this compound. The inhibition of uptake by salicyl hydroxamic acid (SHAM) and iodoacetate (IAA), and the retention of intracellular substrate against large chemical gradients indicate a coupling of energy to this system. The system shows high affinity for pentamidine with an average K m value of 2.68 μM. Structural specificity in relationship to varying drug affinities for this transport site and the role it might play in drug resistance are discussed.