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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Recent Progress in Development of Non-ATP Competitive Small-Molecule Inhibitors of Protein Kinases

Author(s): Alex Kiselyov, Konstantin V. Balakin, Sergey E. Tkachenko and Nikolay P. Savchuk

Volume 6, Issue 6, 2006

Page: [711 - 717] Pages: 7

DOI: 10.2174/138955706777435698

Price: $65


The majority of marketed and late stage development kinase inhibitors are reported to be ATPcompetitive. As a result, many promising drug candidates display non-specific activity that results in undesired physiological effects. There is growing interest towards non-ATP competitive kinase inhibitors, as they are expected to yield highly specific and efficacious molecules devoid of non-mechanistic toxicity. Recent developments in this area are summarized in our review.

Keywords: Protein kinases, Tyrosine kinases, Serine/threonine kinases, Non-ATP competitive inhibitor, Allosteric binding, Library design

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