| Literature DB >> 26815195 |
Brian K Albrecht1, Victor S Gehling1, Michael C Hewitt1, Rishi G Vaswani1, Alexandre Côté1, Yves Leblanc1, Christopher G Nasveschuk1, Steve Bellon1, Louise Bergeron1, Robert Campbell1, Nico Cantone1, Michael R Cooper1, Richard T Cummings1, Hariharan Jayaram1, Shivangi Joshi1, Jennifer A Mertz1, Adrianne Neiss1, Emmanuel Normant1, Michael O'Meara1, Eneida Pardo1, Florence Poy1, Peter Sandy1, Jeffrey Supko1, Robert J Sims1, Jean-Christophe Harmange1, Alexander M Taylor1, James E Audia1.
Abstract
In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promising approach to regulate the expression of important disease-relevant genes, including MYC, BCL-2, and NF-κB. Here we describe the identification and characterization of a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor that attenuates BET-dependent gene expression in vivo, demonstrates antitumor efficacy in an MV-4-11 mouse xenograft model, and is currently undergoing human clinical trials for hematological malignancies (CPI-0610).Entities:
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Year: 2016 PMID： 26815195 DOI： 10.1021/acs.jmedchem.5b01882
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446