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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Published in:J Med Chem
Main Authors: 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
Language:Inglês
Published: 2015
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Article
Online Access: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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