Journal article icon

Journal article

Quantitative, wide-spectrum kinase profiling in live cells for assessing the effect of cellular ATP on target engagement

Abstract:

For kinase inhibitors, intracellular target selectivity is fundamental to pharmacological mechanism. Although a number of acellular techniques have been developed to measure kinase binding or enzymatic inhibition, such approaches can fail to accurately predict engagement in cells. Here we report the application of an energy transfer technique that enabled the first broad-spectrum, equilibrium-based approach to quantitatively profile target occupancy and compound affinity in live cells. Using ...

Expand abstract
Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

Actions


Access Document


Files:
Publisher copy:
10.1016/j.chembiol.2017.10.010

Authors


Corona, CR More by this author
Wilkinson, J More by this author
Zimprich, CA More by this author
Hartnett, JR More by this author
Expand authors...
Publisher:
Cell Press Publisher's website
Journal:
Cell Chemical Biology Journal website
Volume:
25
Issue:
2
Pages:
206-214.e11
Publication date:
2017-11-22
Acceptance date:
2017-10-24
DOI:
ISSN:
2451-9456
Pubs id:
pubs:806819
URN:
uri:ee5bde05-d271-4fdc-b14c-f3aff02be40f
UUID:
uuid:ee5bde05-d271-4fdc-b14c-f3aff02be40f
Local pid:
pubs:806819

Terms of use


Metrics



If you are the owner of this record, you can report an update to it here: Report update to this record

TO TOP