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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Recent Progress in the Identification and Clinical Evaluation of Inhibitors of the Mitotic Kinesin KSP

Author(s): Steven D. Knight and Cynthia A. Parrish

Volume 8, Issue 10, 2008

Page: [888 - 904] Pages: 17

DOI: 10.2174/156802608784911626

Price: $65

Abstract

Kinesin spindle protein (KSP), a mitotic kinesin responsible for bipolar spindle establishment and maintenance, is currently the target of intense research for the development of novel anticancer therapeutics. Several inhibitors of KSP have progressed into clinical trials and many others are in preclinical development. A majority of these inhibitors are ATP-uncompetitive and bind in an allosteric loop L5 binding pocket, but recently, inhibitors with an alternative mechanism of action (ATP-competitive) have also been identified and characterized. In this review, an update of the clinical trial results with ATP-uncompetitive KSP inhibitors is provided and recent progress in the identification of additional KSP inhibitors is discussed.

Keywords: Kinesin, inhibitor, kinesin spindle protein, KSP, Eg5, cancer


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