Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
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DOI: 10.1021/acs.jmedchem.0c00566
Abstract: The bromodomain and extraterminal domain (BET) family of epigenetic regulators comprises four proteins (BRD2, BRD3, BRD4, BRDT), each containing tandem bromodomains. To date, small molecule inhibitors of these proteins typically bind all eight bromodomains of… read more here.
Keywords: anti inflammatory; extraterminal domain; inflammatory antiproliferative; domain bet ... See more keywords
Bromodomain and Extraterminal Domain (BET) Protein Inhibition Hinders Glioblastoma Progression by Inducing Autophagy-Dependent Differentiation
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DOI: 10.3390/ijms24087017
Abstract: Glioblastoma multiforme (GBM) is the most common and aggressive type of malignant primary brain tumor, and it is characterized by a high recurrence incidence and poor prognosis due to the presence of a highly heterogeneous… read more here.
Keywords: protein inhibition; domain bet; gbm; differentiation ... See more keywords