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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Current Inhibitors of Checkpoint Kinase 2

Author(s): T. N.T. Nguyen and J. J. Tepe

Volume 18 , Issue 28 , 2011

Page: [4368 - 4374] Pages: 7

DOI: 10.2174/092986711797200390

Price: $65

Abstract

Checkpoint kinase 2 is a serine/threonine protein which functions as an important transducer in apoptosis or DNA repair following activation by DNA damage. Inhibition of checkpoint kinase 2 is thought to sensitize p53-mutated or p53-deficient cancerous cells but protect normal tissue following DNA-damage caused by ionizing radiation or chemotherapeutic agents. The development of checkpoint kinase inhibitors for the treatment of cancer has therefore been a major objective in drug discovery over the past decade. Several inhibitors have been co-crystallized in the active site of checkpoint kinase 2 revealing important features of effective inhibitors. Some of these inhibitors have entered clinical trials in the last decade. This review describes and discusses the most recent inhibitors of checkpoint kinase 2 as reported in the literature, including an evaluation of biological activity.

Keywords: Checkpoint kinase 2, chemotherapy, kinase inhibitors, DNA, DNA-damage, ionizing radiation, chemotherapeutic agents, cancer, serine/threonine protein, biological activity


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