5HYN
 
 | | Structure of Human Polycomb Repressive Complex 2 (PRC2) with oncogenic histone H3K27M peptide | | 分子名称: | H3K27M, Histone-lysine N-methyltransferase EZH2, JARID2 K116me3, ... | | 著者 | Zhang, Y, Justin, N, Wilson, J.R, Gamblin, S.J. | | 登録日 | 2016-02-01 | | 公開日 | 2016-05-11 | | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | | 主引用文献 | Structural basis of oncogenic histone H3K27M inhibition of human polycomb repressive complex 2.
Nat Commun, 7, 2016
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5K0M
 | | Targeting the PRC2 complex through a novel protein-protein interaction inhibitor of EED | | 分子名称: | (3R,4S)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-{4-[4-(methylsulfonyl)piperazin-1-yl]phenyl}pyrrolidin-3-amine, Polycomb protein EED | | 著者 | Jakob, C.G, Bigelow, L.J, Zhu, H, Sun, C. | | 登録日 | 2016-05-17 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | | 主引用文献 | The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.
Nat. Chem. Biol., 13, 2017
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5KJH
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5KKL
 | | Structure of ctPRC2 in complex with H3K27me3 and H3K27M | | 分子名称: | ALA-ALA-ARG-M3L-SER-ALA-PRO-ALA, Putative uncharacterized protein,Histone H3.1 peptide,Zinc finger domain-containing protein, S-ADENOSYLMETHIONINE, ... | | 著者 | Jiao, L, Liu, X. | | 登録日 | 2016-06-21 | | 公開日 | 2017-04-19 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.94 Å) | | 主引用文献 | Response to Comment on "Structural basis of histone H3K27 trimethylation by an active polycomb repressive complex 2".
Science, 354, 2016
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5GSA
 | | EED in complex with an allosteric PRC2 inhibitor | | 分子名称: | Histone-lysine N-methyltransferase EZH2, N-(furan-2-ylmethyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine, Polycomb protein EED | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-08-15 | | 公開日 | 2017-02-01 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.49 Å) | | 主引用文献 | An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of
Nat. Chem. Biol., 13, 2017
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5H14
 | | EED in complex with an allosteric PRC2 inhibitor EED666 | | 分子名称: | 2-[3-(3,5-dimethylpyrazol-1-yl)-4-nitro-phenyl]-3,4-dihydro-1H-isoquinoline, GLYCEROL, Histone-lysine N-methyltransferase EZH2, ... | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-10-08 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
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5H15
 | | EED in complex with PRC2 allosteric inhibitor EED709 | | 分子名称: | (3R,4S)-1-[(2-methoxyphenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine, Histone-lysine N-methyltransferase EZH2, Polycomb protein EED | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-10-08 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.27 Å) | | 主引用文献 | Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
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5H19
 | | EED in complex with PRC2 allosteric inhibitor EED162 | | 分子名称: | 5-(furan-2-ylmethylamino)-9-(phenylmethyl)-8,10-dihydro-7H-[1,2,4]triazolo[3,4-a][2,7]naphthyridine-6-carbonitrile, Histone-lysine N-methyltransferase EZH2, Polycomb protein EED | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-10-08 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
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5H13
 | | EED in complex with PRC2 allosteric inhibitor EED396 | | 分子名称: | 4-azanylidene-2-(3-methoxy-4-propan-2-yloxy-phenyl)-6,7-dihydro-[1,3]benzodioxolo[6,5-a]quinolizine-3-carbonitrile, GLYCEROL, PRASEODYMIUM ION, ... | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-10-08 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
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5H17
 | | EED in complex with PRC2 allosteric inhibitor EED210 | | 分子名称: | (3R,4aS,10aS)-6-methoxy-3-[(3-methoxyphenyl)methyl]-1-methyl-3,4,4a,5,10,10a-hexahydro-2H-benzo[g]quinoline, Histone-lysine N-methyltransferase EZH2, Polycomb protein EED | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-10-08 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
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5H25
 | | EED in complex with PRC2 allosteric inhibitor compound 11 | | 分子名称: | 5-(2-fluorophenyl)-2,3-dihydroimidazo[2,1-a]isoquinoline, Histone-lysine N-methyltransferase EZH2, Polycomb protein EED | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-10-14 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.88 Å) | | 主引用文献 | Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
J. Med. Chem., 60, 2017
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5H24
 | | EED in complex with PRC2 allosteric inhibitor compound 8 | | 分子名称: | 5-(furan-2-ylmethylamino)-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrile, Histone-lysine N-methyltransferase EZH2, Polycomb protein EED | | 著者 | Zhao, K, Zhao, M, Luo, X, Zhang, H. | | 登録日 | 2016-10-14 | | 公開日 | 2017-01-25 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
J. Med. Chem., 60, 2017
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5BJS
 | | Apo ctPRC2 in an autoinhibited state | | 分子名称: | Histone-lysine N-methyltransferase EZH2, Polycomb protein SUZ12, Polycomb Protein EED, ... | | 著者 | Bratkowski, M.A, Liu, X. | | 登録日 | 2016-10-22 | | 公開日 | 2017-06-14 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.189 Å) | | 主引用文献 | Polycomb repressive complex 2 in an autoinhibited state.
J. Biol. Chem., 292, 2017
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5TQR
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5TTW
 | | Crystal Structure of EED in Complex with UNC4859 | | 分子名称: | Polycomb protein EED, SULFATE ION, UNC4859, ... | | 著者 | The, J, Barnash, K.D, Brown, P.J, Edwards, A.M, Bountra, C, Frye, S.V, James, L.I, Arrowsmith, C.H. | | 登録日 | 2016-11-04 | | 公開日 | 2017-01-11 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.74 Å) | | 主引用文献 | Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.
ACS Comb Sci, 19, 2017
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5U62
 | | Crystal structure of EED in complex with H3K27Me3 peptide and 6-(benzo[d][1,3]dioxol-4-ylmethyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine | | 分子名称: | (6S)-6-[(2H-1,3-benzodioxol-4-yl)methyl]-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine, GLYCEROL, Histone-lysine N-methyltransferase EZH2, ... | | 著者 | Bussiere, D, Shu, W. | | 登録日 | 2016-12-07 | | 公開日 | 2017-01-11 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
J. Med. Chem., 60, 2017
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5U69
 | | Polycomb protein EED in complex with inhibitor: (3R,4S)-1-[(2-methoxyphenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine | | 分子名称: | (3R,4S)-1-[(2-methoxyphenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine, Polycomb protein EED | | 著者 | Jakob, C.G, Zhu, H. | | 登録日 | 2016-12-07 | | 公開日 | 2017-03-15 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.28 Å) | | 主引用文献 | SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Bioorg. Med. Chem. Lett., 27, 2017
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5U5T
 | | Crystal structure of EED in complex with H3K27Me3 peptide and 3-(benzo[d][1,3]dioxol-4-ylmethyl)piperidine-1-carboximidamide | | 分子名称: | (3R)-3-[(2H-1,3-benzodioxol-4-yl)methyl]piperidine-1-carboximidamide, Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, ... | | 著者 | Bussiere, D, Shu, W. | | 登録日 | 2016-12-07 | | 公開日 | 2017-01-11 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
J. Med. Chem., 60, 2017
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5U6D
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5U8F
 | | Polycomb protein EED in complex with inhibitor: (3R,4S)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine | | 分子名称: | (3R,4S)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine, Polycomb protein EED | | 著者 | Jakob, C.G, Zhu, H. | | 登録日 | 2016-12-14 | | 公開日 | 2017-03-15 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.343 Å) | | 主引用文献 | SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Bioorg. Med. Chem. Lett., 27, 2017
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5U8A
 | | Polycomb protein EED in complex with inhibitor: (3R,4S)-1-[(2-bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine | | 分子名称: | (3R,4S)-1-[(2-bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine, Polycomb protein EED | | 著者 | Jakob, C.G, Zhu, H. | | 登録日 | 2016-12-14 | | 公開日 | 2017-03-15 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.45 Å) | | 主引用文献 | SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Bioorg. Med. Chem. Lett., 27, 2017
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5WUK
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5VK3
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5XTZ
 | | Crystal structure of GAS41 YEATS bound to H3K27ac peptide | | 分子名称: | ACETATE ION, THR-LYS-ALA-ALA-ARG-ALY-SER-ALA-PRO-ALA, YEATS domain-containing protein 4 | | 著者 | Li, H.T, Zhao, D. | | 登録日 | 2017-06-21 | | 公開日 | 2018-06-27 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.105 Å) | | 主引用文献 | Gas41 links histone acetylation to H2A.Z deposition and maintenance of embryonic stem cell identity.
Cell Discov, 4, 2018
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5XVW
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