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Covalent-fragment screening of BRD4 identifies a ligandable site orthogonal to the acetyl-lysine binding sites

BRD4, a member of the bromodomain and extraterminal domain (BET) family, has emerged as a promising epigenetic target in cancer and inflammatory disorders. All reported BET family ligands bind within the bromodomain acetyl-lysine binding sites and competitively inhibit BET protein interaction with a...

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Bibliografski detalji
Izdano u:ACS Chem Biol
Glavni autori: Olp, Michael D., Sprague, Daniel J., Goetz, Christopher J., Kathman, Stefan G., Wynia-Smith, Sarah L., Shishodia, Shifali, Summers, Steven B., Xu, Ziyang, Statsyuk, Alexander V., Smith, Brian C.
Format: Artigo
Jezik:Inglês
Izdano: 2020
Teme:
Online pristup:https://ncbi.nlm.nih.gov/pmc/articles/PMC7271629/
https://ncbi.nlm.nih.gov/pubmed/32149490
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acschembio.0c00058
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