Article
Esterase mutation is a mechanism of resistance to antimalarial compounds.
Nature communications - 20 Jan 2017
Istvan Eva S, Mallari Jeremy P, Corey Victoria C, Dharia Neekesh V, Marshall Garland R, Winzeler Elizabeth A, Goldberg Daniel E
Abstract excerpt
Pepstatin is a potent peptidyl inhibitor of various malarial aspartic proteases, and also has parasiticidal activity. Activity of pepstatin against cultured Plasmodium falciparum is highly variable depending on the commercial source. Here we identify a minor contaminant (pepstatin butyl ester) as the active anti-parasitic principle. We synthesize a series of derivatives and characterize an analogue (pepstatin...
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