METHOD FOR THE IDENTIFICATION OF ACTIVE SITE PROTEASE INACTIVATORS

摘要

A method for identifying active site inhibitors of a target protease. Kinetic assays are employed to identify peptide substrates that tightly bind to the active site of the target protease but are not easily cleaved. These noncleavable but tightly binding substrates are structurally modified to yield inhibitory compounds that, additionally, exhibit apparent specificity for a transition state or ground state configuration of the protease.