BET inhibitors are a class of drugs that reversibly bind the bromodomains of Bromodomain and Extra-Terminal motif (BET) proteins BRD2, BRD3, BRD4, and BRDT, and prevent protein-protein interaction between BET proteins and acetylated histones and transcription factors.[1][2]
^Garnier JM, Sharp PP, Burns CJ (February 2014). "BET bromodomain inhibitors: a patent review". Expert Opinion on Therapeutic Patents. 24 (2): 185–99. doi:10.1517/13543776.2014.859244. PMID 24261714. S2CID 24647727.
^Shi J, Vakoc CR (June 2014). "The mechanisms behind the therapeutic activity of BET bromodomain inhibition". Molecular Cell. 54 (5): 728–36. doi:10.1016/j.molcel.2014.05.016. PMC 4236231. PMID 24905006.
BETinhibitors in combination with γ-secretase inhibitors for T cell acute lymphoblastic leukemia and BRAF-inhibitor (vemurafenib) for BRAF-inhibitor...
stage. Small molecule inhibitors of non-BET bromodomain proteins BRD7 and BRD9 have also been developed. Chromodomain BETinhibitor BRD2 BRD3 BRD4 BRD7...
inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific protein BRDT in mammals. BETinhibitors structurally...
morpholine-containing chemical compound that is a potent inhibitor of numerous proteins, and a strong inhibitor of phosphoinositide 3-kinases (PI3Ks). It is generally...
in clinical trials. Overall, there is a mean survival of 6–9 months. BETinhibitor RESERVED, INSERM US14-- ALL RIGHTS. "Orphanet: NUT midline carcinoma"...
able to prevent successful interaction between BET proteins and acetylated histones. Using a BETinhibitor can reduce the over expression of bromodomain...
R. Herrman, B. Merkely, M. Borgman, S.E. Nissen. Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of...
(MUFJ) keiretsu. Mitsubishi-Tanabe Pharmaceuticals developed the first BETinhibitor molecules. In August 2014, the company announced three-year research...
small-molecule inhibitor 9-ME-1. This bumped inhibitor was found to have an IC50 of 200nM and over 100-fold specificity for the L/V BET mutant BD over...
member of the BET (bromodomain and extra terminal domain) family, which also includes BRD2, BRD3, and BRDT. BRD4, similar to other BET family members...
that occurs after histone hyperacetylation in elongating spermatids. BETinhibitors such as JQ1 block the region of BRDT responsible for chromatin binding...
A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein (CETP). They are intended to reduce the risk of atherosclerosis...
GM, Lock RB, Liu T (May 2016). "The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression...
molecular pathologies. P300 inhibition has shown to inhibit the deleterious effects of DUX4 BETinhibitors have been shown to reduce DUX4 expression. Antioxidants...
"Direct interaction of c-Myc with Smad2 and Smad3 to inhibit TGF-beta-mediated induction of the CDK inhibitor p15(Ink4B)". Molecular Cell. 9 (1): 133–43. doi:10...
reformulation of an AstraZeneca castoff rival Takeda's new heartburn drug? Here's a $26M bet on yes". endpts.com. "Linaprazan glurate". Cinclus Pharma....
functional overlap with close homolog BRD3. BRD2 function is blocked by BETinhibitors. BRD2 has been shown to interact with E2F2, and many transcription factors...
lower doses compared to their inhibitor analogues. Some PROTACs have been shown to be more selective than their inhibitor analogues, reducing off-target...
hepatocellular carcinoma. It is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and also inhibits AXL and RET. It was discovered and developed...
Alzheimer's. The company sold the rights to Faldaprevir, a HCV protease inhibitor to Trek Therapeutics. In July 2016, the company sold the commercialisation...
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