Selective inhibitors of bromodomain BD1 and BD2 of BET proteins modulate radiation‐induced profibrotic fibroblast responses
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DOI: 10.1002/ijc.33989
Abstract: Radiotherapy can induce various adverse effects including fibrosis in cancer patients. Radiation‐induced aberrant expression of profibrotic genes has been associated with dysregulated epigenetic mechanisms. Pan‐BET (bromodomain and extraterminal domain) inhibitors, such as JQ1 and I‐BET151,… read more here.
Keywords: bet proteins; bd2; ibet bd2; radiation induced ... See more keywords
Structure-Based Discovery and Optimization of Furo[3,2-c]pyridin-4(5H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors.
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DOI: 10.1021/acs.jmedchem.2c00100
Abstract: Pan-bromodomain and extra terminal (Pan-BET) inhibitors show profound efficacy but exhibit pharmacology-driven toxicities in clinical trials. The development of domain-selective BET inhibitors to separate efficacy and toxicity is urgently needed. Herein, we report a series… read more here.
Keywords: furo pyridin; extra terminal; bd2; bet inhibitors ... See more keywords
Discovery of the First BRD4 Second Bromodomain (BD2)-Selective Inhibitors.
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DOI: 10.1021/acs.jmedchem.4c02516
Abstract: Pan-BD2 inhibitors have been shown to retain an antileukemia effect and display less dose-limiting toxicities than pan-BET inhibitors. However, it is necessary to consider the potential off-target toxicity associated with the inhibition of four BET… read more here.
Keywords: bd2; brd4 bd2; first brd4; selectivity ... See more keywords