New Endicott and Noble paper

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

Aude Echalier, Alison J. Hole, Graziano Lolli, Jane A. Endicott, and Martin E. M. Noble

ACS Chem. Biol., 2014, 9 (6), pp 1251–1256   DOI: 10.1021/cb500135f

Using 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, Jane and Martin's group find that different activation states of a particular CDK may differ from each other as much as different CDKs in the same activation state. They 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 Date: March 26, 2014

Last modified: Mon, 27 Jul 2015 13:43:12 BST