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Current Medicinal Chemistry

Editor-in-Chief

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

Farnesyl Protein Transferase Inhibition: A Novel Approach to Anti-tumor

Author(s): A. K. Ganguly, R. J. Doll and V.M. Girijavallabhan

Volume 8, Issue 12, 2001

Page: [1419 - 1436] Pages: 18

DOI: 10.2174/0929867013372021

Price: $65

Abstract

Farnesyl protein transferase (FPT) inhibition is an interesting and promising approach to non-cytotoxic anticancer therapy. Research in this area has resulted in several orally active compounds that are currently in clinical evaluation. This review focuses on FPT inhibitors in clinical trials and concentrates on the benzocycloheptapyridine class, with details on the discovery and development of SCH 66336, currently in Phase II clinical trials.

Keywords: Farnesyl Protein Transferase Inhibition, Anti-tumor Therapy, farnesyl protein transferase, Farnesylation, Geranlylgeranylation, carboxymethyl transferase, FPT Enzyme Assay, COS Assay, Pharmacokinetic Assay (PK), Potent FPT Inhibitors


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