Identification of Enzyme Inhibitors Using Combinatorial Libraries

摘要

Potent enzyme inhibitors have long been recognized as powerful tools for assessing thenphysiological roles of enzymes and have led to the therapeutic drugs able to modulate their activities innvivo. However, to be valuable tools such inhibitors should be selective so that they do not interfere withnother members of the particular enzyme family. Combinatorial chemistry has proven to be a novelnapproach for the identification of molecules with a desired selectivity profile from the libraries of severalnmillion compounds. In recent years it has been extensively used in conjunction with computationalnmethods for the development of potent inhibitors of therapeutically interesting targets. This reviewndescribes the various structurally diverse enzyme inhibitors identified by screening combinatorialnlibraries of peptides and small organic molecules.