2025年1月14日,复旦大学陈飞、中国科学院分子细胞科学卓越创新中心姜海、同济大学张鹏共同通讯在Nature Chemical Biology(IF=13)在线发表题为“Catalytic-independent functions of the Integrator–PP2A complex (INTAC) confer sensitivity to...
Roeder博士 (Arnold and Mabel Beckman Professor) 和张思聪博士(research associate)在Nature Structural & Molecular Biology上发表了文章Resistance of estrogen receptor function to BET bromodomain inhibition is mediated by transcriptional...
BET bromodomain inhibition targets both c-MYC and IL7R in high-risk acute lymphoblastic leukemia. Blood. 2012; 120 :2843–52.Ott C.J., Kopp N., Bird L., Paranal R.M., Qi J., Bowman T., Rodig S.J., Kung A.L., Bradner J.E., Weinstock D.M. Bet bromodomain...
To assess the therapeutic effect of combined inhibition of ATR kinase and BET protein we cultured the melanoma cell lines A375 and MeWo in the presence of the ATR inhibitor (ATRI) VE821 and/or RVX2135.15,19 Both compounds were anti- proliferative as assessed by microscopy, CellTiter Glo (...
体内研究中,(+)-JQ1(50 mg/kg, i.p.)处理NMC 797移植瘤小鼠,发现JQ1抑制肿瘤生长,肿瘤体积减小,而且FDG吸收明显减少。[1] 参考文献 [1] Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature, 468(7327): 1067-1073 (2010). ...
产品活性:(+)-JQ-1 (JQ1) 是一种有效特异性的可逆 BET bromodomain 抑制剂,抑制 BRD4(1/2) 的 IC50 分别为 77 nM 和 33 nM。(+)-JQ-1 激活自噬 (autophagy)。 体外:(+)-JQ-1 代表溴结构域 BET 家族的一种有效、高度特异性和 Kac 竞争性抑制剂。(+)- JQ-1 (100 nM,48 h) 促进鳞状分化,...
产品活性:(+)-JQ-1 (JQ1) 是一种有效特异性的可逆 BET bromodomain 抑制剂,抑制 BRD4(1/2) 的 IC50 分别为 77 nM 和 33 nM。(+)-JQ-1 激活自噬 (autophagy)。 体外:(+)-JQ-1 代表溴结构域 BET 家族的一种有效、高度特异性和 Kac 竞争性抑制剂。(+)- JQ-1 (100 nM,48 h) 促进鳞状分化,...
R. The mechanisms behind the therapeutic activity of BET bromodomain inhibition. Mol. Cell 54, 728–736 (2014). Article CAS PubMed Google Scholar Ernst, J. & Kellis, M. Discovery and characterization of chromatin states for systematic annotation of the human genome. Nat. Biotechnol. 28, ...
BET(bromodomain and extraterminal)蛋白家族是bromodomain蛋白超家族的一个亚类。人类基因中有40余种不同的蛋白质编码60多种bromodomain,根据序列的同源性,bromodomain蛋白家族可分成8个亚类,其中BET蛋白家族是一个特殊群体,其特点是N末端包含2个保守的bromodomain(BD1和BD...
PD-1 blockade combined with BET bromodomain inhibition enhances T-cell activation and effector activity Figure 2. PD-1 blockade and BET bromodomain inhibition promote increased activation and effector capacity of tumor-infiltratin...