Specific inhibition of CK2α from an anchor outside the active site

P. Brear(University of Cambridge), Claudia De Fusco(University of Cambridge), Kathy Hadje Georgiou(University of Cambridge), Nicola J. Francis-Newton(University of Cambridge), Christopher J. Stubbs(University of Cambridge), Hannah F. Sore(University of Cambridge), Ashok R. Venkitaraman(University of Cambridge), Chris Abell(University of Cambridge), David R. Spring(University of Cambridge), Marko Hyvönen(University of Cambridge)
Chemical Science
January 1, 2016
Cited by 73Open Access
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Abstract

CAM4066, a specific CK2α kinase inhibitor, is anchored in the cryptic αD pocket outside the active site and inserts a “warhead” into the active site, blocking ATP binding and thereby inhibiting the kinase.


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