Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

The bromodomain containing proteins TRIM24 (Tripartite motif containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are involved in the epigenetic regulation of gene expression and have been implicated in human cancer. Overexpression of TRIM24 correlates with poor patient...

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Veröffentlicht in:J Med Chem
Hauptverfasser: Palmer, Wylie S., Poncet-Montange, Guillaume, Liu, Gang, Petrocchi, Alessia, Reyna, Naphtali, Subramanian, Govindan, Theroff, Jay, Yau, Anne, Kost-Alimova, Maria, Bardenhagen, Jennifer P., Leo, Elisabetta, Shepard, Hannah E., Tieu, Trang N., Shi, Xi, Zhan, Yanai, Zhao, Shuping, Barton, Michelle C., Draetta, Giulio, Toniatti, Carlo, Jones, Philip, Do, Mary Geck, Andersen, Jannik N.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2015
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Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4755933/
https://ncbi.nlm.nih.gov/pubmed/26061247
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.5b00405
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