Recent progress in development of non-ATP competitive small-molecule inhibitors of protein kinases

The majority of marketed and late stage development kinase inhibitors are reported to be ATP-competitive. 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...

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Bibliographic Details
Published inMini reviews in medicinal chemistry Vol. 6; no. 6; p. 711
Main Authors Kiselyov, Alex, Balakin, Konstantin V, Tkachenko, Sergey E, Savchuk, Nikolay P
Format Journal Article
LanguageEnglish
Published Netherlands 01.06.2006
Subjects
Adenosine Triphosphate - chemistry
Binding, Competitive
Drug Design
Humans
Protein Conformation
Protein Kinase Inhibitors - chemistry
Protein Kinases - chemistry
Protein Kinases - drug effects
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Summary:The majority of marketed and late stage development kinase inhibitors are reported to be ATP-competitive. 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.
ISSN:1389-5575
DOI:10.2174/138955706777435698