Figure 4: PfPARE hydrolyzes and activates an ester-containing prodrug.
From: Esterase mutation is a mechanism of resistance to antimalarial compounds
Concentration-responses against 3D7 asexual parasites (right) and structures (left) of compounds from the MDTIP consortium16. EC50 values were measured with a flow cytometry-based assay. Parasite strains are labelled black (3D7), blue (pfpare wild-type allelic exchange), green (pfpare L357P allelic exchange) and orange (pfpare S179T allelic exchange). Inhibition data were fit to a sigmoidal concentration-response curve. (a) MMV011438, (b) MMV021735, (c) MMV030666. In a, F-test; P<0.0001 for S179T or L357P compared to Wt. Error bars show s.d.±indicates standard errors calculated for the biological triplicates of the experiment shown. N=2.
