An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

Nature Chemical Biology

Volumn 13, Issue 4, 2017, Pages 381-388

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

^a Novartis Institutes for Biomedical Research   (China)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; EED 226; EMBRYONIC ECTODERM DEVELOPMENT PROTEIN; HISTONE H3; POLYCOMB REPRESSIVE COMPLEX 2; PROTEIN INHIBITOR; TAZEMETOSTAT; UNCLASSIFIED DRUG; EED226; HISTONE; LYSINE; SULFONE; TRIAZOLE DERIVATIVE;

ALLELE; ALLOSTERISM; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; CLINICAL TRIAL (TOPIC); COMPETITIVE INHIBITION; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DIFFUSE LARGE B CELL LYMPHOMA; DRUG BINDING SITE; DRUG CONFORMATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG TARGETING; FEMALE; GAIN OF FUNCTION MUTATION; HISTONE METHYLATION; HUMAN; HUMAN TISSUE; IC50; INHIBITORY DOSE; ISOTHERMAL TITRATION CALORIMETRY; MOUSE; NONHUMAN; PRIORITY JOURNAL; STOICHIOMETRY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; TUMOR VOLUME; TUMOR XENOGRAFT; UPREGULATION; WD REPEAT; ANIMAL; ANTAGONISTS AND INHIBITORS; BAGG ALBINO MOUSE; BINDING SITE; CELL PROLIFERATION; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; DRUG SCREENING; METABOLISM; MOLECULAR MODEL; NEOPLASMS, EXPERIMENTAL; NUDE MOUSE; PATHOLOGY; TUMOR CELL CULTURE; TUMOR CELL LINE;

ALLOSTERIC REGULATION; ANIMALS; ANTINEOPLASTIC AGENTS; BINDING SITES; CELL LINE, TUMOR; CELL PROLIFERATION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; HISTONES; HUMANS; LYSINE; MICE; MICE, INBRED BALB C; MICE, NUDE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEOPLASMS, EXPERIMENTAL; POLYCOMB REPRESSIVE COMPLEX 2; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES; TRIAZOLES; TUMOR CELLS, CULTURED;

EID: 85010896299     PISSN: 15524450     EISSN: 15524469     Source Type: Journal    
DOI: 10.1038/nchembio.2304     Document Type: Article

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