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An Inhibitor's-Eye View of the ATP-Binding Site of CDKs in Different Regulatory States

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.

Publication metadata

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


DOI: 10.1021/cb500135f


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Funder referenceFunder name
European Commission (PROKINASE Project)
083113/Z/07/AWellcome Trust