http://www.sciencedirect.com/science/article/pii/S0006291X17301389
CG13250, a novel bromodomain inhibitor, suppresses proliferation of multiple myeloma cells in an orthotopic mouse model
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Natsuki Imayoshia, Makoto Yoshiokab, Jay Chauhanc, Susumu Nakatad, Yuki Todaa, Steven Fletcherc,
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Jeffrey W. Strovelb, Kazuyuki Takataa, Eishi Ashiharaa, ,
- a Department of Clinical and Translational Physiology, Kyoto Pharmaceutical University, Kyoto, Japan
- b ConverGene LLC, Gaithersburg, MD, USA
- c Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, USA
- d Department of Clinical Oncology, Kyoto Pharmaceutical University, Kyoto, Japan
Received 12 January 2017, Accepted 18 January 2017, Available online 20 January 2017
• A novel bromodomain inhibitor CG13250 suppresses MM cell proliferation.• CG13250 decreases C-MYC expression, resulting in the induction of apoptosis.• CG13250 prolongs the survivals of MM-bearing mice.
In text: JQ-1
[12] and I-BET762
[13] were the first BET inhibitors to be described and these compounds suppress MM cell proliferation
[14] ;
[15]. Other BET inhibitors described to date include PFI-1,
RVX-208, and OTX015
[9] ;
[16]. By conducting chemical screening against BRD4 and subsequent chemical optimization, we developed a novel bromodomain inhibitor CG13250.
Unlike previously described BET inhibitors, it has a quinolinone core and displayed high affinity and specificity to BET proteins. In this study, we investigated the inhibitory effects of CG13250 on the proliferation of MM cells.
Didn't see Zen-3694 mentioned in this one, though.