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

23 December 2019, Version 1

Abstract

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.

Keywords

Cyclin Dependent Kinases
CDK
cyclin
target engagement assay
selectivity
residence time
nanoBRET
BRET
energy transfer

Supplementary materials

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CDK Paper Supplement ChemRxiv 12182019
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Table S3
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Table S4
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Table S5
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Version History

Dec 23, 2019 Version 1

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The content is available under CC BY NC ND 4.0 [opens in a new tab]

DOI

10.26434/chemrxiv.11401419.v1
D O I: 10.26434/chemrxiv.11401419.v1 [opens in a new tab]

Funding

National Institute of Diabetes and Digestive and Kidney Diseases
U24DK116204
Illuminating Function of the Understudied Druggable Kinome
https://app.dimensions.ai/details/grant/grant.7029421 [opens in a new tab]
Wellcome Trust
106169/Z/14/Z
A UK Hub to Catalyse Open Target Discovery.
https://app.dimensions.ai/details/grant/grant.4580835 [opens in a new tab]

Author’s competing interest statement

no conflict of interest

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