JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific protein BRDT in mammals. BET inhibitors structurally similar to JQ1 are being tested in clinical trials for a variety of cancers including NUT midline carcinoma . [ 1 ]

2021年3月15日 · A chemical combinatorial screening of JQ1 with around 1900 compounds aimed at finding effective small molecule combination therapies with BETi revealed PI3K inhibitors to be the most potent ...

2023年5月1日 · JQ1: JQ1 was the first and most well-characterized BRD4 inhibitor reported in 2010. JQ1 is a thieno-triazolo-1,4-diazepine that displaces BET proteins from chromatin by competitively binding to acetyl-lysine recognition motifs or bromodomains (Fig. 2).

2020年3月10日 · Our results suggest that BET protein inhibitor JQ1 prohibits the malignant progression of GC cells by downregulating chromatin accessibility and inactivating RUNX2/NID1 signaling. The clinical...

2016年6月13日 · JQ1 reduced TNBC growth in vitro and in vivo and inhibited xenograft vascularization. These findings identify that BETi dually targets angiogenesis and the hypoxic response, an effective...

2018年9月1日 · JQ1 as a first-in-class potent and selective inhibitor of the BRD4 signaling pathway is widely used for tumor biology studies. It was found that JQ1 could potently reduce cancer cell viability in vitro and in vivo.

2024年4月1日 · JQ1, a small molecule inhibitor of BRD4, is superior in synergistic treatment with PDT. The nanocomplex exhibited enhanced immunotherapeutic effects and inhibited distant tumour growth.

In our study, we found that JQ1 can inhibit the expression of NSC markers Nestin and ciliary neurotrophic factor and promote GSC differentiation to astrocytes under proliferative conditions. The role of JQ1 in promoting GSCs needs further study.

JQ1 is a member of the class of thienotriazolodiazepines that is the tert-butyl ester of [(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetic acid. An inhibitor of bromodomain-containing protein 4 that exhibits anti …

JQ1 induces adipose tissue wasting without affecting skeletal muscle mass and function. Timeline and schedule of (A) long-term experiment: mice were exposed for 20 weeks to high fat diet (HFD) or standard diet (SD) and then treated with 20 mg/kg/day JQI or vehicle for 2 weeks, and (F) mid-term experiment: mice were exposed for 10 weeks to HFD or SD and then treated with 10 mg/kg/day JQ1 or ...

2021年1月1日 · JQ1 is a BRD4 inhibitor that has been widely studied in cancer research. It displaces BET bromodomains from chromatin and interferes with BRD4 function, leading to cell cycle arrest and the induction of apoptosis (Filippakopoulos et al., 2010; Shi et al., 2018).

JQ1 may be a new drug for oral squamous cell carcinoma treatment. The present study aimed to evaluate whether bromodomain 4 (BRD4) is expressed in Cal27 cells and to assess the effect of JQ1 on cell proliferation, apoptosis, invasion and BRD4, C …

2019年7月16日 · JQ1 is a bromodomain inhibitor, which selectively binds to the amino-terminal twin bromodomains of BET proteins 10. JQ1 treatment displaces BRD4, inhibiting its ability to read acetylated...

2016年12月2日 · JQ1 is a small molecule that interferes with transcriptional regulators, such as BRD4, by preventing them from interacting with acetylated regions of the genome and thus inhibiting the transcriptional activation of BRD4 target genes.

2014年1月23日 · JQ1, a chemical compound that inhibits MYC expression is therapeutically effective in preclinical animal models in midline carcinoma, and Burkitt’s lymphoma (BL). Here we show that JQ1 does not inhibit MYC expression to a similar extent in all tumor cells.

2022年10月11日 · Chromatin reader protein that recognizes and binds acetylated histones and plays a key role in transmission of epigenetic memory across cell divisions and transcription regulation (PubMed:20871596, PubMed:23086925, PubMed:23317504, PubMed:29176719, PubMed:29379197).

The selective small molecule inhibitor JQ1, which binds competitively to bromodomains, has been reported to exhibit anti‑proliferative effects in various types of cancer.

2010年9月24日 · Here we report a cell-permeable small molecule (JQ1) that binds competitively to acetyl-lysine recognition motifs, or bromodomains.

2025年2月1日 · JQ1 induces adipose tissue depletion preserving skeletal muscle mass and strength. JQ1-induced adipose tissue loss does not alter systemic glucose and improves lipid homeostasis. JQ1 exerts a lipolytic action, inducing ATGL and HSL transcripts in …

In the present study, we investigated the effects of JQ1, a bromodomain and extraterminal-bromodomain inhibitor, on cell growth, and messenger RNA (mRNA) and protein levels of PD-L1 in renal cell carcinoma primary culture cells, and prostate, liver, and lung cancer cell lines.