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Structural origins of AGC protein kinase inhibitor selectivities: PKA as a drug discovery tool
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Espen Åberg
Published/Copyright:
September 8, 2012
Abstract
The era of structure-based protein kinase inhibitor design began in the early 1990s with the determination of crystal structures of protein kinase A (PKA, or cyclic AMP-dependent kinase). Although many other protein kinases have since been extensively characterized, PKA remains a prototype for studies of protein kinase active conformations. It serves well as a model for the structural properties of AGC subfamily protein kinases, clarifying inhibitor selectivity profiles. Its reliable expression, constitutive activity, simple domain structure, and reproducible crystallizability have also made it a useful surrogate for the discovery of inhibitors of both established and emerging AGC kinase targets.
Received: 2012-7-9
Accepted: 2012-8-22
Published Online: 2012-09-08
Published in Print: 2012-10-01
©2012 by Walter de Gruyter Berlin Boston
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- Masthead
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