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Lookup NU author(s): Dr Alison Hole, Professor Jane Endicott, Professor Martin NobleORCiD
This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).
We have used a chemically diverse panel of kinase inhibitors to assess the chemical similarity of the ATP-binding sites of cyclin-dependent kinase (CDK) subfamily members in a range of activation states. Using this approach, we find that different activation states of a particular CDK may differ from each other as much as different CDKs in the same activation state. We also find that inhibitors discriminate more effectively among CDK family members in their monomeric state than in their cyclin-bound state, providing direct evidence for the belief that selective binding to inactive kinase states might be more readily achieved than selective binding to active states.
Author(s): Echalier A, Hole AJ, Lolli G, Endicott JA, Noble MEM
Publication type: Article
Publication status: Published
Journal: ACS Chemical Biology
Year: 2014
Volume: 9
Issue: 6
Pages: 1251-1256
Print publication date: 20/06/2014
Online publication date: 26/03/2014
Acceptance date: 26/03/2014
Date deposited: 07/07/2015
ISSN (print): 1554-8929
ISSN (electronic): 1554-8937
Publisher: American Chemical Society
URL: http://dx.doi.org/10.1021/cb500135f
DOI: 10.1021/cb500135f
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