Cambridge Open Engage home
What is Cambridge Open Engage?
How to Submit
Browse
About
News [opens in a new tab]

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

Title
Description
Actions
Title
CDK Paper Supplement ChemRxiv 12182019
Description
Actions
Title
Table S3
Description
Actions
Title
Table S4
Description
Actions
Title
Table S5
Description
Actions

Comments

Comments are not moderated before they are posted, but they can be removed by the site moderators if they are found to be in contravention of our Commenting Policy [opens in a new tab] - please read this policy before you post. Comments should be used for scholarly discussion of the content in question. You can find more information about how to use the commenting feature here [opens in a new tab] .
This site is protected by reCAPTCHA and the Google Privacy Policy [opens in a new tab] and Terms of Service [opens in a new tab] apply.

Version History

Dec 23, 2019 Version 1

Metrics

3,776
1,218
0
Views
Downloads
Citations

License

CC logo
CC
BY logo
BY
NC logo
NC
ND logo
ND
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

Share