An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.-论文-万方医学网

作者： Wei,Qi ^[1] ; Kehao,Zhao ^[1] ; Justin,Gu ^[1] ; Ying,Huang ^[1] ; Youzhen,Wang ^[1] ; Hailong,Zhang ^[1] ; Man,Zhang ^[1] ; Jeff,Zhang ^[1] ; Zhengtian,Yu ^[1] ; Ling,Li ^[1] ; Lin,Teng ^[1] ; Shannon,Chuai ^[1] ; Chao,Zhang ^[1] ; Mengxi,Zhao ^[1] ; HoMan,Chan ^[1] ; Zijun,Chen ^[1] ; Douglas,Fang ^[1] ; Qi,Fei ^[1] ; Leying,Feng ^[1] ; Lijian,Feng ^[1] ; Yuan,Gao ^[1] ; Hui,Ge ^[1] ; Xinjian,Ge ^[1] ; Guobin,Li ^[1] ; Andreas,Lingel ^[2] ; Ying,Lin ^[1] ; Yueqin,Liu ^[1] ; Fangjun,Luo ^[1] ; Minlong,Shi ^[1] ; Long,Wang ^[1] ; Zhaofu,Wang ^[1] ; Yanyan,Yu ^[1] ; Jue,Zeng ^[1] ; Chenhui,Zeng ^[1] ; Lijun,Zhang ^[1] ; Qiong,Zhang ^[1] ; Shaolian,Zhou ^[1] ; Counde,Oyang ^[1] ; Peter,Atadja ^[1] ; En,Li ^[1]

作者单位： Novartis Institutes for BioMedical Research, Shanghai, China. ^[1] Novartis Institutes for BioMedical Research, Emeryville, California, USA. ^[2]

主题词别构调节(Allosteric Regulation);动物(Animals);抗肿瘤药(Antineoplastic Agents);结合部位(Binding Sites);细胞系, 肿瘤(Cell Line, Tumor);细胞增殖(Cell Proliferation);剂量效应关系, 药物(Dose-Response Relationship, Drug);药物筛选试验, 抗肿瘤(Drug Screening Assays, Antitumor);女(雌)性(Female);组蛋白类(Histones);人类(Humans);赖氨酸(Lysine);小鼠(Mice);小鼠, 近交BALB C(Mice, Inbred BALB C);小鼠, 裸(Mice, Nude);模型, 分子(Models, Molecular);分子结构(Molecular Structure);肿瘤, 实验性(Neoplasms, Experimental);构效关系(Structure-Activity Relationship);砜类(Sulfones);三唑类(Triazoles);肿瘤细胞, 培养的(Tumor Cells, Cultured)

DOI 10.1038/nchembio.2304

PMID 28135235

发布时间 2018-11-13

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An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.

Nature chemical biology

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An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.

Nature chemical biology

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Nature chemical biology

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