Abstract
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
Mini-Reviews in Medicinal Chemistry
Title: Recent Progress in Development of Non-ATP Competitive Small-Molecule Inhibitors of Protein Kinases
Volume: 6 Issue: 6
Author(s): Alex Kiselyov, Konstantin V. Balakin, Sergey E. Tkachenko and Nikolay P. Savchuk
Affiliation:
Keywords: Protein kinases, Tyrosine kinases, Serine/threonine kinases, Non-ATP competitive inhibitor, Allosteric binding, Library design
Abstract: 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.
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Cite this article as:
Kiselyov Alex, Balakin V. Konstantin, Tkachenko E. Sergey and Savchuk P. Nikolay, Recent Progress in Development of Non-ATP Competitive Small-Molecule Inhibitors of Protein Kinases, Mini-Reviews in Medicinal Chemistry 2006; 6 (6) . https://dx.doi.org/10.2174/138955706777435698
DOI https://dx.doi.org/10.2174/138955706777435698 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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