High-throughput kinase profiling as a platform for drug discovery.
To fully exploit the potential of kinases as drug targets, novel strategies for the efficient discovery of inhibitors are required. In contrast to the traditional, linear process of inhibitor discovery, high-throughput kinase profiling enables a parallel approach by interrogating compounds against hundreds of targets in a single screen. Compound potency and selectivity are determined simultaneously, providing a choice of targets to pursue that is guided by the quality of lead compounds available, rather than by target biology alone.
Goldstein
David M
DM
Roche Palo Alto, 3431 Hillview Avenue, R6-201, Palo Alto, California 94304, USA.
Gray
Nathanael S
NS
Zarrinkar
Patrick P
PP
D015195:Drug Design; D006801:Humans; D040081:Protein Array Analysis; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D011494:Protein Kinases / Q000737:chemistry / Q000378:metabolism*
D047428:Protein Kinase Inhibitors; D011494:Protein Kinases