Apr 23, 2014 · Here we show that AR-signalling-competent human CRPC cell lines are preferentially sensitive to bromodomain and extraterminal (BET) inhibition. BRD4 physically …

Dec 28, 2023 · Androgen receptor (AR) is the primary target for treating prostate cancer (PCa), which inevitably progresses due to drug-resistant mutations. Bromodomain-containing protein …

Sep 16, 2019 · Bromodomain (BRD) and extra-terminal motif (BET) protein inhibitors have been shown to attenuate AR signaling in metastatic castration-resistant prostate cancer and to …

Sep 26, 2023 · Upregulated BRD4 is associated with HIF-1α and acetylated histones and binds to AR promoter, activating AR transcription. Selective BRD4 inhibitor JQ1 suppresses BRD4 …

Feb 14, 2017 · BRD4 can also physically interact with androgen receptor (AR), and disruption of this interaction by a BET inhibitor can abrogate BRD4 localization to AR target loci and AR …

Feb 19, 2019 · Previous studies have demonstrated that BRD4 can promote the transcriptional activities of oncogenic factors in prostate cancer by physically interacting with the N‐terminal …

In this study, AR activation in dehydroepiandrosterone- and letrozole-induced rat PCOS ovaries coincided with a marked increase of a chromatin acetylation ‘‘reader’’ BRD4. Further …

Sep 1, 2021 · E2F1 and BRD4 are critical for activating an AR-repressed, t-NEPC lineage plasticity program. BETi is a promising approach to block this program.

Jan 5, 2022 · Here, we designed and synthesized a series of BRD4-PROTACs based on a dual BET/PLK1 inhibitor WNY0824, and the optimal molecule WWL0245 could degrade BRD4 …

Jan 22, 2020 · Analyses of RNA expression and chromatin immunoprecipitation followed by sequencing revealed that ABBV-744 displaced BRD4 from AR-containing super-enhancers …