Ontology highlight
ABSTRACT:
SUBMITTER: Istvan ES
PROVIDER: S-EPMC5263872 | biostudies-literature | 2017 Jan
REPOSITORIES: biostudies-literature
Istvan Eva S ES Mallari Jeremy P JP Corey Victoria C VC Dharia Neekesh V NV Marshall Garland R GR Winzeler Elizabeth A EA Goldberg Daniel E DE
Nature communications 20170120
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 hexyl ester) with low nanomolar activity. By selecting resistant parasite mutants, we f ...[more]