Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold

[Image: see text] Recent reports have highlighted the dual bromodomains of TAF1 (TAF1(1,2)) as synergistic with BET inhibition in cellular cancer models, engendering interest in TAF/BET polypharmacology. Here, we examine structure activity relationships within the BI-2536 PLK1 kinase inhibitor scaff...

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Bibliografiset tiedot
Julkaisussa:ACS Med Chem Lett
Päätekijät: Remillard, David, Buckley, Dennis L., Seo, Hyuk-Soo, Ferguson, Fleur M., Dhe-Paganon, Sirano, Bradner, James E., Gray, Nathanael S.
Aineistotyyppi: Artigo
Kieli:Inglês
Julkaistu: American Chemical Society 2019
Linkit:https://ncbi.nlm.nih.gov/pmc/articles/PMC6792166/
https://ncbi.nlm.nih.gov/pubmed/31620231
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00243
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