Inhibition of SmPOP activity and anti-schistosomal effect of synthetic SmPOP inhibitors.

a The IC50 values were determined in a kinetic activity assay with recombinant SmPOP or HsPOP and the fluorogenic substrate Z-Gly-Pro-AMC at pH 8.0. The mean values ± S.D. of three replicates are given.
b Induction of phenotype alterations by the inhibitors was determined with NTS in culture. The inhibitors were tested at 10 μM and 1 μM concentrations, and the resulting phenotypes, arising as a function of time and concentration, were graded I to III, with grade I being the most severe (see Materials and Methods).
c Y-29794 oxalate: 2-[[8-(Dimethylamino)octyl]thio]-6-(1-methylethyl)-3-pyridinyl-2-thienylmethanone oxalate
d SUAM 14746: 3-([4-[2-(E)-styrylphenoxy]butanoyl]-L-4-hydroxyprolyl)thiazolidine).
e Peptidic inhibitors with reactive aldehyde (CHO) or chloromethyl ketone (CMK) warheads (see Materials and Methods).
Inhibition of SmPOP activity and anti-schistosomal effect of synthetic SmPOP inhibitors.