Compensatory RNA polymerase 2 loading determines the efficacy and transcriptional selectivity of JQ1 in Myc-driven tumorsdoi:10.1038/leu.2016.182Inhibition of bromodomain and extraterminal motif (BET) proteins such as BRD4 bears great promise for cancer treatment and its efficacy has been frequently ...
selectivity in targeting tumor cells, particularly in hematological tumors where their efficacy was linked to Myc downregulation.11,15–17 Indeed, in multiple myelo- mas bearing chromosomal rearrangements that bring the coding region of c-Myc under the transcriptional control of the IgH locus, BRD4 ...
However, BET inhibitors lack the selectivity for individual BET proteins, thereby limiting their scope in selectively targeting the physiologically relevant BRD4 protein to efficiently inhibit c-Myc expression (Zengerle et al., 2015). Show abstract Make your best BET: The emerging role of BET ...
Compensatory RNA polymerase 2 loading determines the efficacy and transcriptional selectivity of JQ1 in Myc-driven tumors.Inhibition of bromodomain and extraterminal motif (BET) proteins such as BRD4 bears great promise for cancer treatment and its efficacy has been frequently attributed to Myc ...
As a class, ‘BET’ inhibitors disrupt binding of bromodomain and extra-terminal motif (BET) proteins, BRD2, BRD3, BRD4 and BRDT, to acetylated histones preventing recruitment of RNA polymerase 2 to enhancers and promoters, especially super-enhancers, to