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.
Abbott Laboratories, Global Pharmaceutical Research and Development, Cancer Research Department R47S, 100 Abbott Park Road, Abbott Park, IL 60064, USA. yan.luo@abbott.com
Yan
Y
Luo
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