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, 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.
Kiselyov
Alex
A
ChemDiv, Inc., San Diego, CA 92121, USA. ask@chemdiv.com
Balakin
Konstantin V
KV
Tkachenko
Sergey E
SE
Savchuk
Nikolay P
NP
D000255:Adenosine Triphosphate / Q000737:chemistry*; D001667:Binding, Competitive; D015195:Drug Design; D006801:Humans; D011487:Protein Conformation; D047428:Protein Kinase Inhibitors / Q000737:chemistry*; D011494:Protein Kinases / Q000737:chemistry* / Q000187:drug effects*
D047428:Protein Kinase Inhibitors; D000255:Adenosine Triphosphate; D011494:Protein Kinases