Enhanced selectivity for inhibition of analog-sensitive protein kinases through scaffold optimization

C Zhang, KM Shokat

Index: Zhang, Chao; Shokat, Kevan M. Tetrahedron, 2007 , vol. 63, # 26 p. 5832 - 5838

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Citation Number: 8

Abstract

The ability to inhibit any protein kinase of interest with a small molecule is enabled by a combination of genetics and chemistry. Genetics is used to modify the active site of a single kinase to render it distinct from all naturally occurring kinases. Next, organic synthesis is used to develop a small molecule, which does not bind to wild-type kinases but is a potent inhibitor of the engineered kinase. This approach, termed chemical genetics, has been ...