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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...
Autores principales: | 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. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Royal Society of Chemistry
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5909127/ https://www.ncbi.nlm.nih.gov/pubmed/29732121 http://dx.doi.org/10.1039/c7sc02536j |
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