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