Structural specificity of chloroquine-hematin binding related to inhibition of hematin polymerization and parasite growth

…, A Dorn, H Matile, AK Bhattacharjee…

Index: Vippagunta, Sudha Rani; Dorn, Arnulf; Matile, Hugues; Bhattacharjee, Apurba K.; Karle, Jean M.; Ellis, William Y.; Ridley, Robert G.; Vennerstrom, Jonathan L. Journal of Medicinal Chemistry, 1999 , vol. 42, # 22 p. 4630 - 4639

Full Text: HTML

Citation Number: 149

Abstract

Considerable data now support the hypothesis that chloroquine (CQ)-hematin binding in the parasite food vacuole leads to inhibition of hematin polymerization and parasite death by hematin poisoning. To better understand the structural specificity of CQ-hematin binding, 13 CQ analogues were chosen and their hematin binding affinity, inhibition of hematin polymerization, and inhibition of parasite growth were measured. As determined by ...