Current Medicinal Chemistry - Anti-Cancer Agents

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

DOI: 10.2174/1568011054866928

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

Page: [561 - 573] Pages: 13

  • * (Excluding Mailing and Handling)

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