Perspectives in the design of small molecule enzyme inhibitors as useful drugs

Abstract

An irreversible inhibitor is often assessed as a potential drug on the basis of its specificity towards a target enzyme in vitro. This is inadequate because in vivo the enzyme may be re-synthesized and the inhibitor may react with other major body constituents, e.g. glutathione. Guidelines are given for selecting the class of inhibitor to be studied for use in a particular clinical area.