Article
Turning a protein kinase on or off from a single allosteric site via disulfide trapping.
Proceedings of the National Academy of Sciences of the United States of America - 12 Apr 2011
Sadowsky Jack D, Burlingame Mark A, Wolan Dennis W, McClendon Christopher L, Jacobson Matthew P, Wells James A
Abstract excerpt
There is significant interest in identifying and characterizing allosteric sites in enzymes such as protein kinases both for understanding allosteric mechanisms as well as for drug discovery. Here, we apply a site-directed technology, disulfide trapping, to interrogate structurally and functionally how an allosteric site on the Ser/Thr kinase, 3-phosphoinositide-dependent kinase 1 (PDK1)--the...
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