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26 Apr 2017 Keywords: PAX3-FOXO1, BET bromodomains, Rhabdomyosarcoma mutational burden indicating that the fusion gene is the primary oncogenic driver. .. FP-RMS would be selectively vulnerable to inhibition of these SE .. the R statistical package drc (https://cran.r-project.org/web/packages/drc/drc.pdf). 24 Sep 2010 Bromodomain-containing proteins are of substantial biological A selective and potent inhibitor for the BET sub-family of bromodomains. 30 Jan 2017 MYC is a major cancer driver but is documented to be a difficult therapeutic target the BET (bromodomains and extraterminal domain) family of . highly selective and potent inhibitor of PI3K, particularly of the ? isoform of 4 Oct 2011 Inhibition of BET bromodomain–promoter interactions and . BET-Bromodomain Inhibition Potently Suppresses MYC Gene Expression. .. in human neuroblastoma and is functionally believed to be a driver of this disease (23). . (2010) Selective inhibition of BET bromodomains. . 40. Masthead (PDF) 24 Sep 2010 doi:10.1038/nature09504. Selective inhibition of BET bromodomains. Panagis Filippakopoulos1*, Jun Qi2*, Sarah Picaud1*, Yao Shen3, 17 Apr 2017 characterization of a novel BET family bromodomain inhibitor, ABBV-075. . ABBV-075 is a potent and selective BET family bromodomain protein inhibitor. .. factors is often highlighted as the primary driver of their activity in. Inhibition of BET proteins by the small-molecule inhibitor I-BET affects the I-BET selectively inhibits genes that follow an “analog”-like activation pattern while 1 Jan 2016 Enter your search terms www.thno.org Submit search form. PDF . Unexpectedly, transcriptome profiling revealed that JQ1 selectively downregulated These findings indicate that BET bromodomain inhibition is a promising .. as a candidate oncogenic driver of epithelial ovarian carcinoma and provide Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24. Selective inhibition of BET bromodomains. Filippakopoulos P(1), Qi J, 19 Mar 2014 Treatment with JQ1, a BET bromodomain inhibitor, reduces cell viability to be a potential oncogenic driver in osteosarcoma, depending on its