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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Identification of Enzyme Inhibitors Using Combinatorial Libraries

Author(s): S. Batra, T. Srinivasan, S. K. Rastogi and B. Kundu

Volume 9 , Issue 3 , 2002

Page: [307 - 319] Pages: 13

DOI: 10.2174/0929867023371120

Price: $65


Potent enzyme inhibitors have long been recognized as powerful tools for assessing the physiological roles of enzymes and have led to the therapeutic drugs able to modulate their activities in vivo. However, to be valuable tools such inhibitors should be selective so that they do not interfere with other members of the particular enzyme family. Combinatorial chemistry has proven to be a novel approach for the identification of molecules with a desired selectivity profile from the libraries of several million compounds. In recent years it has been extensively used in conjunction with computational methods for the development of potent inhibitors of therapeutically interesting targets. This review describes the various structurally diverse enzyme inhibitors identified by screening combinatorial libraries of peptides and small organic molecules.

Keywords: Enzyme Inhibitors, PROTEASE PLASMEPSIN (PLM) II, carboxypeptidases, kallikrein

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