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
Current Medicinal Chemistry
Title: Current Inhibitors of Checkpoint Kinase 2
Volume: 18 Issue: 28
Author(s): T. N.T. Nguyen and J. J. Tepe
Affiliation:
Keywords: Checkpoint kinase 2, chemotherapy, kinase inhibitors, DNA, DNA-damage, ionizing radiation, chemotherapeutic agents, cancer, serine/threonine protein, biological activity
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.
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Cite this article as:
N.T. Nguyen T. and J. Tepe J., Current Inhibitors of Checkpoint Kinase 2, Current Medicinal Chemistry 2011; 18 (28) . https://dx.doi.org/10.2174/092986711797200390
DOI https://dx.doi.org/10.2174/092986711797200390 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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