Quantitative, wide-spectrum kinase profiling in live cells for assessing the effect of cellular ATP on target engagement
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
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- Cell Press Publisher's website
- Cell Chemical Biology Journal website
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- Vasta et al.
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Copyright © 2017 The Authors. Published by Elsevier Ltd.
This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
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