Selectivity assessment of kinase inhibitors: strategies and challenges.
Most small-molecule kinase inhibitors are ATP competitive, which render them more likely to cross-inhibit other kinases in the same family or even kinases from other families. Assessing compound selectivity is therefore critical for drug development. Recent development of several cutting-edge technologies enabled rapid advances in kinase selectivity assessment and greatly facilitated the industrial drug discovery process.
Luo
Yan
Y
Abbott Laboratories, Global Pharmaceutical Research and Development, Cancer Research Department R47S, 100 Abbott Park Road, Abbott Park, IL 60064, USA. yan.luo@abbott.com
D000818:Animals; D001665:Binding Sites; D015195:Drug Design; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000737:chemistry*; D011494:Protein Kinases / Q000737:chemistry*; D013329:Structure-Activity Relationship
D047428:Protein Kinase Inhibitors; D011494:Protein Kinases