New lead generation strategies for protein kinase inhibitors - fragment based screening approaches.
The protein kinase superfamily represents both an enormous opportunity and a unique challenge for drug discovery. Protein kinases play central roles in the cellular economy and it is well known that a large number of diseases involve aberrant protein kinase activity. This review discusses how fragment based screening strategies, such as virtual screening, NMR and high-throughput X-ray crystallography are being employed to identify new chemo-types to produce the next generation of protein kinase inhibitors.
Gill
Adrian
A
Astex Technology, 436 Cambridge Science Park, Milton Road, Cambridge, CB4 0QA, UK. a.gill@astex-technology.com
D000818:Animals; D001665:Binding Sites; D018360:Crystallography, X-Ray; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry*; D006801:Humans; D008958:Models, Molecular; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000737:chemistry; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases