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Quinine Dimers Are Potent Inhibitors of the Plasmodium falciparum Chloroquine Resistance Transporter and Are Active against Quinoline-Resistant P. falciparum

Hrycyna, Christine A.; Summers, Robert; Lehane, Adele; Pires, Marcos M.; Namanja, Hilda; Bohn, Kelsey; Kuriakose, Jerrin; Ferdig, Michael T; Henrich, Philipp P.; Fidock, David A; Kirk, Kiaran; Chmielewski, Jean; Martin, Rowena

Description

Chloroquine (CQ) resistance in the human malaria parasite Plasmodium falciparum is primarily conferred by mutations in the "chloroquine resistance transporter" (PfCRT). The resistance-conferring form of PfCRT (PfCRTCQR) mediates CQ resistance by effluxing the drug from the parasite's digestive vacuole, the acidic compartment in which CQ exerts its antiplasmodial effect. PfCRTCQR can also decrease the parasite's susceptibility to other quinoline drugs, including the current antimalarials quinine...[Show more]

CollectionsANU Research Publications
Date published: 2013
Type: Journal article
URI: http://hdl.handle.net/1885/21236
Source: ACS chemical biology
DOI: 10.1021/cb4008953

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