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

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

Volume: 8 Issue: 10

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

Affiliation:

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

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.

Cite this article as:

Knight D. Steven and Parrish A. Cynthia, Recent Progress in the Identification and Clinical Evaluation of Inhibitors of the Mitotic Kinesin KSP, Current Topics in Medicinal Chemistry 2008; 8 (10) . https://dx.doi.org/10.2174/156802608784911626