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Use of the NP-40 detergent-mediated assay in discovery of inhibitors of beta-hematin crystallization.


ABSTRACT: The protozoan parasite responsible for malaria affects over 500 million people each year. Current antimalarials have experienced decreased efficacy due to the development of drug-resistant strains of Plasmodium spp., resulting in a critical need for the discovery of new antimalarials. Hemozoin, a crystalline by-product of heme detoxification that is necessary for parasite survival, serves as an important drug target. The quinoline antimalarials, including amodiaquine and chloroquine, act by inhibiting the formation of hemozoin. The formation of this crystal does not occur spontaneously, and recent evidence suggests crystallization occurs in the presence of neutral lipid particles located in the acidic digestive vacuole of the parasite. To mimic these conditions, the lipophilic detergent NP

SUBMITTER: Sandlin RD 

PROVIDER: S-EPMC3122397 | biostudies-literature | 2011 Jul

REPOSITORIES: biostudies-literature