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Comprehensive Survey of CDK Inhibitor Selectivity in Live Cells with Energy Transfer Probes

preprint
submitted on 18.12.2019 and posted on 23.12.2019 by Carrow Wells, Jim Vasta, Cesear R. Corona, Jennifer Wilkinson, Chad A. Zimprich, Morgan R. Ingold, Julie E. Pickett, David Drewry, Kathryn Maria Pugh, Kilian Huber, Mei Cong, Poncho Meisenheimer, Timothy M. Willson, Matthew B. Robers
A panel of cell-permeable energy transfer probes has been developed to quantify target occupancy for all 21 CDKs in live, intact cells. Here we present the first comprehensive evaluation of intracellular isozyme potency and selectivity for a collection of 46 clinically-advanced CDKi’s and tool molecules. Here we provide a broadly applicable method for evaluating the selectivity of chemical matter for CDKs in living cells, and present a refined set of tool molecules to study CDK function.

Funding

Illuminating Function of the Understudied Druggable Kinome

National Institute of Diabetes and Digestive and Kidney Diseases

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A UK Hub to Catalyse Open Target Discovery.

Wellcome Trust

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History

Email Address of Submitting Author

Carrow.Wells@unc.edu

Institution

Univerisity of North Carolina at Chapel Hill

Country

USA

ORCID For Submitting Author

0000-0003-4799-6792

Declaration of Conflict of Interest

no conflict of interest

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