Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition

Allele-specific chemical genetics enables selective inhibition within families of highly-conserved proteins. The four BET (bromodomain & extra-terminal domain) proteins – BRD2, BRD3, BRD4 and BRDT bind acetylated chromatin via their bromodomains and regulate processes such as cell proliferation...

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Udgivet i:Chem Sci
Main Authors: Runcie, A. C., Zengerle, M., Chan, K.-H., Testa, A., van Beurden, L., Baud, M. G. J., Epemolu, O., Ellis, L. C. J., Read, K. D., Coulthard, V., Brien, A., Ciulli, A.
Format: Artigo
Sprog:Inglês
Udgivet: Royal Society of Chemistry 2018
Fag:
Chemistry
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5909127/
https://ncbi.nlm.nih.gov/pubmed/29732121
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/c7sc02536j
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