
Targeting c-Myc: JQ1 as a promising option for c-Myc-amplified ... - PubMed
2018年4月10日 · The bromodomain inhibitor JQ1, which targets c-Myc, exerts anti-tumor activity in multiple cancers. However, the role of JQ1 in ESCC remains unknown. In this study, we reported that JQ1 had potent anti-proliferative effects on ESCC cells in both time- and dose-dependent manners by inducing cell cycle arrest at G1 phase, cell apoptosis, and the ...
BET bromodomain inhibition as a therapeutic strategy to target c-Myc ...
2011年9月16日 · Using a selective small-molecule bromodomain inhibitor, JQ1, we identify BET bromodomain proteins as regulatory factors for c-Myc. BET inhibition by JQ1 downregulates MYC transcription, followed by genome-wide downregulation of Myc-dependent target genes.
Achieving clinical success with BET inhibitors as anti-cancer agents ...
2021年3月15日 · RNA interference screening detected a dependency of acute myeloid leukaemia (AML) models on BRD4 expression, and JQ1 treatment led to anti-cancer effects in in vitro and in vivo settings by ...
MYC activity at enhancers drives prognostic transcriptional …
2024年3月7日 · Our short-term treatment with the BET inhibitor JQ1 showed that this inhibitor blocks RNAPII recruitment at MYC-bound enhancers without changing MYC protein levels as has previously been...
Regulation of MYC Expression and Differential JQ1 Sensitivity in …
High level MYC expression is associated with almost all human cancers. 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 ...
Targeting MYC dependence in cancer by inhibiting BET …
Lack of systemic effects was not attributable to an inability of (+)-JQ1 to repress murine MYC, as treatment of the mouse cell lines EL4 and RAW264.7 with (+)-JQ1 resulted in substantial MYC suppression (Fig. S5E). These data demonstrate significant in vivo antitumor activity linked to BET inhibition and suggest a potential therapeutic use for ...
Colorectal cancer inhibition by BET inhibitor JQ1 is MYC …
2022年2月1日 · JQ1 altered MYC in only two among four CRC cell lines. This MYC-independence found in CT26 was confirmed in vivo by PCR and immunohistochemistry. The main explanation of the JQ1 anticancer effect was an increase in apoptosis. The investigation of its impact on the tumor microenvironment did not show significant effects.
Colorectal cancer inhibition by BET inhibitor JQ1 is MYC ... - PubMed
JQ1 altered MYC in only two among four CRC cell lines. This MYC-independence found in CT26 was confirmed in vivo by PCR and immunohistochemistry. The main explanation of the JQ1 anticancer effect was an increase in apoptosis.
Targeting c-Myc: JQ1 as a promising option for c-Myc-amplified ...
2018年4月10日 · In this study, we reported that JQ1 had potent anti-proliferative effects on ESCC cells in both time- and dose-dependent manners by inducing cell cycle arrest at G1 phase, cell apoptosis, and the mesenchymal-epithelial transition.
BET protein inhibitor JQ1 attenuates Myc-amplified MCC tumor …
BET Inhibitor JQ1 abolishes c-Myc expression and represses primary MCC cell proliferation. Targeting c-Myc by the BET inhibitor JQ1 has demonstrated efficient suppression of c-Myc expression as well as antitumor activity in many types of human cancer both in vitro and in vivo (28, 32). We therefore decided to examine the effects of growth ...