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Chlorpheniramine analogues reverse chloroquine resistance in plasmodium falciparum by inhibiting PfCRT

Deane, Karen; Summers, Robert; Lehane, Adele; Martin, Rowena; Barrow, Russell


The emergence and spread of malaria parasites that are resistant to chloroquine (CQ) has been a disaster for world health. The antihistamine chlorpheniramine (CP) partially resensitizes CQ-resistant (CQR) parasites to CQ but possesses little intrinsic antiplasmodial activity. Mutations in the parasite's CQ resistance transporter (PfCRT) confer resistance to CQ by enabling the protein to transport the drug away from its site of action, and it is thought that resistance-reversers such as CP exert...[Show more]

CollectionsANU Research Publications
Date published: 2014
Type: Journal article
Source: ACS Medicinal Chemistry Letters
DOI: 10.1021/ml5000228


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