Abstract
Background Chloroquine (CQ) resistance in P. falciparum is strongly linked to mutations in the gene pfcrt that gives rise to the protein, PfCRT (P. falciparum chloroquine resistance transporter), located in the parasite’s digestive vacuole (DV) membrane [1]. In CQ resistant (CQR) strains, accumulation of CQ is reduced in the DV due to increased efflux [2], relative to CQ sensitive (CQS) malaria.
Highlights
Chloroquine (CQ) resistance in P. falciparum is strongly linked to mutations in the gene pfcrt that gives rise to the protein, PfCRT (P. falciparum chloroquine resistance transporter), located in the parasite’s digestive vacuole (DV) membrane [1]
We have developed a class of molecules, termed Reversed Chloroquine compounds (RCQs), that are hybrids made up of a chloroquine (CQ) like moiety, and a chemosensitizer (Reversal Agent, RA) against CQ resistant (CQR) in malaria [3]
We report on an expanded set of RCQ entities
Summary
Progress in the development of Reversed Chloroquine molecules as antimalarial therapy Steven J Burgess2*, Jane Xu-Kelly, Katherine Liebmann, Bornface Gunsaru, Westin Morrill, David H Peyton1,2*. From Parasite to Prevention: Advances in the understanding of malaria Edinburgh, UK. From Parasite to Prevention: Advances in the understanding of malaria Edinburgh, UK. 20-22 October 2010
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