X-Ray Crystallographic Studies of CDK2, a Basis for Cyclin-Dependent Kinase Inhibitor Design in Anti-Cancer Drug Research

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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X-Ray Crystallographic Studies of CDK2, a Basis for Cyclin-Dependent Kinase Inhibitor Design in Anti-Cancer Drug Research



Anti-Cancer Agents in Medicinal Chemistry, 3(1): 15-23.

Author(s): Pascal Furet.

Affiliation: Novartis, WKL-136.P.12, CH-4002 Basel, Switzerland

Abstract

Inhibition of cyclin-dependent kinases is a theme of major interest in current anti-cancer agents research. Different classes of chemical inhibitors of these enzymes have been identified during the past decade and the structural basis of inhibition has been elucidated by X-ray crystallography studies of one member of the family, CDK2. In this article, we review the structural biology work that has led to a precise knowledge of the interactions between CDK2 and small organic molecules binding to its ATP pocket that are determinant for inhibitory activity. The use of this information to design or optimize CDK inhibitors by molecular modeling is also reviewed.

Keywords:

X-Ray, Crystallographic, CDK2, Cyclin-Dependent, Anti-Cancer Drug.



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Article Details

Volume: 3
Issue Number: 1
First Page: 15
Last Page: 23
Page Count: 9
DOI: 10.2174/1568011033353515
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