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 ...

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...

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.

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.

JQ1, a BRD4 inhibitor, downregulates the expression of PD-L1, which leads to reduced immunosuppression 23-25. Besides, JQ1 inhibits tumor growth by enhancing anti-tumor immunity. Moreover, JQ1 facilitates anti-tumor effects of ICIs.

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).

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.

2022年3月28日 · Compared with the control, JQ1 significantly inhibited tumor growth and prolonged the overall survival of the mice. Besides, JQ1 did not only inhibit tumor growth by enhancing anti-tumor immunity, but also promoted the anti-tumor effect of PD-1 antibody.