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Current Medicinal Chemistry - Anti-Cancer Agents

Editor-in-Chief

ISSN (Print): 1568-0118
ISSN (Online): 1875-5968

An Analysis of the Binding Modes of ATP-Competitive CDK2 Inhibitors as Revealed by X-Ray Structures of Protein-Inhibitor Complexes

Author(s): A. Vulpetti and P. Pevarello

Volume 5, Issue 5, 2005

Page: [561 - 573] Pages: 13

DOI: 10.2174/1568011054866928

Price: $65

Abstract

CDK2 is an attractive target for the design of new therapeutic antitumor agent. Numerous CDK2 inhibitors have been discovered and their crystallographic structures either in complex with CDK2 or CDK2/Cyclin A have been published. This review aims to summarize the publicly available structural characterization of CDK2/(Cyclin A) - ligand complexes and to highlight the similarities among the binding modes of structurally diverse inhibitors.

Keywords: cyclin-dependent kinase, cdk, x-ray, cell cycle, crystal structure, binding mode, adenine scaffold, adenine mimics

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