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

[ Vol. 6 , Issue. 6 ]

Author(s):

Alex Kiselyov, Konstantin V. Balakin, Sergey E. Tkachenko and Nikolay P. Savchuk   Pages 711 - 717 ( 7 )

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

Affiliation:

ChemDiv, Inc. 11558Sorrento Valley Rd., Ste. 5, San Diego, CA 92121, USA.



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