| Autor: |
Robert M. Campbell, Yves Leblanc, James E. Audia, Jennifer A. Mertz, Brian K. Albrecht, Michael R. Cooper, Jeffrey G. Supko, Emmanuel Normant, Florence Poy, Christopher G. Nasveschuk, Richard T. Cummings, Michael C. Hewitt, Adrianne Neiss, Victor S. Gehling, Louise Bergeron, Jean-Christophe Harmange, Peter Sandy, Michael O'Meara, Alexander M. Taylor, Robert J. Sims, Nico Cantone, Eneida Pardo, Alexandre Côté, Shivangi Joshi, Hariharan Jayaram, Rishi G. Vaswani, Steve Bellon |
| Rok vydání: |
2016 |
| Předmět: |
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| Zdroj: |
Journal of Medicinal Chemistry. 59:1330-1339 |
| ISSN: |
1520-4804
0022-2623 |
| Popis: |
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). |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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