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Epigenetic Reader Domain

JQ1 Induces DNA Damage and Apoptosis, and Inhibits Tumor Growth in a Patient-Derived Xenograft Model of Cholangiocarcinoma

21 views | Jul 25 2019

Garcia PL et al. suggested that c-Myc inhibition and several of its transcriptional targets may contribute to the mechanism of action of JQ1 in this tumor type. We conclude that BET inhibitors such as JQ1 warrant further investigation for the treatment of CCA. [Read the Full Post]

A natural compound, aristoyagonine, is identified as a potent bromodomain inhibitor by mid-throughput screening

142 views | Feb 18 2019

Kim YH et al. tested Brd4 inhibitors in gastric cancer cell lines, and found that aristoyagonine exerted cytotoxicity not only in I-BET-762-sensitive cancer cells, but also in I-BET-762-resistant cancer cells. This is the first paper to describe a natural compound as a Brd4 bromodomain inhibitor. [Read the Full Post]

BET Bromodomain Inhibition as a Therapeutic Strategy in Ovarian Cancer by Downregulating FoxM1

485 views | Apr 20 2018

Zhang Z et al. provide a mechanistic rationale for the clinical investigation of BET bromodomain inhibitors in this deadly disease. [Read the Full Post]

Concomitant BET and MAPK blockade for effective treatment of ovarian cancer

492 views | Jan 08 2018

Jing Y et al. supportted concomitant BET and MAPK blockade as an effective therapeutic strategy in ovarian cancer. [Read the Full Post]

The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb

576 views | Nov 27 2017

Lu P et al. suggested that the BET inhibitor OTX015 may be a candidate for anti-HIV-1-latency therapies. [Read the Full Post]

Kinome Profiling Identifies Druggable Targets for Novel Human Cytomegalovirus (HCMV) Antivirals

545 views | Nov 26 2017

Arend KC et al. showed the utility of MIB-MS kinome profiling for identifying existing kinase inhibitors that can potentially be repurposed as novel antiviral drugs. [Read the Full Post]

The inhibition of BET leads to a suppression of osteoclastogenesis

2626 views | Dec 15 2014

Park-Min et al. found the inhibitor of bromo and extra-terminal (BET), I-BET151, can strongly reduce osteocelstogenesis. [Read the Full Post]