Fig. 4.
Counter screen of hits toward ENPEP. (A) Coomassie-Blue–stained SDS-PAGE gel and immunoblot of purified human ENPEP. (B) Michaelis Menten kinetics of Glu-AMC hydrolysis by ENPEP. The inset shows the calculated Km and kcat values. (C) Comparison of hits toward DNPEP in Ang II hydrolysis over ENPEP in Glu-AMC hydrolysis in activity score at 10 µM (sorted by activity scores toward ENPEP). Differences in activity score toward DNPEP over ENPEP (Δactivity score) are shown in Table 1. Hits with Δactivity scores ≤−50%, between −50% and −20%, or ≥−20% were defined as DNPEP-selective, DNPEP-preferential, and dual inhibitors, respectively.