5IJ7
 
 | | Structure of Hs/AcPRC2 in complex with a pyridone inhibitor | | 分子名称: | 5,8-dichloro-2-[(4-ethyl-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-({1-[(2R)-2-hydroxypropanoyl]piperidin-4-yl}oxy)-3,4-dihydroisoquinolin-1(2H)-one, Enhancer of Zeste Homolog 2 (EZH2),Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, ... | | 著者 | Gajiwala, K.S, Brooun, A, Deng, Y.-L, Liu, W. | | 登録日 | 2016-03-01 | | 公開日 | 2016-05-04 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.62 Å) | | 主引用文献 | Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.
Nat Commun, 7, 2016
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4W2R
 | | Structure of Hs/AcPRC2 in complex with 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one | | 分子名称: | 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one, Enhancer of zeste 2 polycomb repressive complex 2 subunit, Polycomb protein EED, ... | | 著者 | Gajiwala, K.S, Brooun, A, Liu, W, Deng, Y, Stewart, A.E. | | 登録日 | 2017-09-25 | | 公開日 | 2017-12-27 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.81 Å) | | 主引用文献 | Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
J. Med. Chem., 61, 2018
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6NQ3
 | | Crystal Structure of a SUZ12-RBBP4-PHF19-JARID2 Heterotetrameric Complex | | 分子名称: | Histone-binding protein RBBP4, PHD finger protein 19, Polycomb protein SUZ12, ... | | 著者 | Chen, S, Jiao, L, Liu, X. | | 登録日 | 2019-01-19 | | 公開日 | 2020-01-29 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.89 Å) | | 主引用文献 | A Dimeric Structural Scaffold for PRC2-PCL Targeting to CpG Island Chromatin.
Mol.Cell, 77, 2020
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5WAI
 | | Crystal Structure of a Suz12-Rbbp4-Jarid2-Aebp2 Heterotetrameric Complex | | 分子名称: | Histone-binding protein RBBP4, Jumonji, AT-rich interactive domain 2, ... | | 著者 | Chen, S, Jiao, L, Liu, X. | | 登録日 | 2017-06-26 | | 公開日 | 2018-03-14 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Unique Structural Platforms of Suz12 Dictate Distinct Classes of PRC2 for Chromatin Binding.
Mol. Cell, 69, 2018
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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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5IJ8
 | | Structure of the primary oncogenic mutant Y641N Hs/AcPRC2 in complex with a pyridone inhibitor | | 分子名称: | 5,8-dichloro-2-[(4-ethyl-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-({1-[(2R)-2-hydroxypropanoyl]piperidin-4-yl}oxy)-3,4-dihydroisoquinolin-1(2H)-one, Enhancer of Zeste Homolog 2 (EZH2),Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, ... | | 著者 | Gajiwala, K.S, Brooun, A, Deng, Y.-L, Liu, W. | | 登録日 | 2016-03-01 | | 公開日 | 2016-05-04 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.99 Å) | | 主引用文献 | Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.
Nat Commun, 7, 2016
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7TD5
 | | Structure of human PRC2-EZH1 containing phosphorylated SUZ12 | | 分子名称: | Histone-lysine N-methyltransferase EZH1, Polycomb protein EED, Polycomb protein SUZ12, ... | | 著者 | Gong, L, Jiao, L, Liu, X. | | 登録日 | 2021-12-30 | | 公開日 | 2022-11-16 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.994 Å) | | 主引用文献 | CK2-mediated phosphorylation of SUZ12 promotes PRC2 function by stabilizing enzyme active site.
Nat Commun, 13, 2022
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6B3W
 | | Structure of Hs/AcPRC2 in complex with 5,8-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one | | 分子名称: | 5,8-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one, Enhancer of zeste 2 polycomb repressive complex 2 subunit,Enhancer of zeste 2 polycomb repressive complex 2 subunit, Polycomb protein EED, ... | | 著者 | Gajiwala, K.S, Brooun, A, Liu, W, Deng, Y, Stewart, A.E. | | 登録日 | 2017-09-25 | | 公開日 | 2017-12-27 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.05 Å) | | 主引用文献 | Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
J. Med. Chem., 61, 2018
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5WAK
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8FYH
 | | G4 RNA-mediated PRC2 dimer | | 分子名称: | G4 RNA, Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH2, ... | | 著者 | Song, J, Kasinath, V. | | 登録日 | 2023-01-26 | | 公開日 | 2023-10-04 | | 実験手法 | ELECTRON MICROSCOPY (3.4 Å) | | 主引用文献 | Structural basis for inactivation of PRC2 by G-quadruplex RNA.
Science, 381, 2023
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5LS6
 | | Structure of Human Polycomb Repressive Complex 2 (PRC2) with inhibitor | | 分子名称: | 1-[(1~{R})-1-[1-[2,2-bis(fluoranyl)propyl]piperidin-4-yl]ethyl]-~{N}-[(4-methoxy-6-methyl-2-oxidanylidene-3~{H}-pyridin-3-yl)methyl]-2-methyl-indole-3-carboxamide, Histone-lysine N-methyltransferase EZH2,Histone-lysine N-methyltransferase EZH2,Histone-lysine N-methyltransferase EZH2, Jarid2 K116me3, ... | | 著者 | Zhang, Y, Justin, N, Chen, S, Wilson, J, Gamblin, S. | | 登録日 | 2016-08-22 | | 公開日 | 2017-02-22 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (3.47 Å) | | 主引用文献 | Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
J. Med. Chem., 59, 2016
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6C24
 | | Cryo-EM structure of PRC2 bound to cofactors AEBP2 and JARID2 in the Extended Active State | | 分子名称: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH2, JARID2-substrate, ... | | 著者 | Kasinath, V, Faini, M, Poepsel, S, Reif, D, Feng, A, Stjepanovic, G, Aebersold, R, Nogales, E. | | 登録日 | 2018-01-06 | | 公開日 | 2018-01-24 | | 最終更新日 | 2019-12-18 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | Structures of human PRC2 with its cofactors AEBP2 and JARID2.
Science, 359, 2018
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6WKR
 | | PRC2-AEBP2-JARID2 bound to H2AK119ub1 nucleosome | | 分子名称: | DNA (314-MER), Histone H2A type 1, Histone H2B 1.1, ... | | 著者 | Kasinath, V, Nogales, E, Beck, C, Sauer, P, Poepsel, S, Kosmatka, J, Faini, M, Toso, D, Aebersold, R. | | 登録日 | 2020-04-16 | | 公開日 | 2021-02-03 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | JARID2 and AEBP2 regulate PRC2 in the presence of H2AK119ub1 and other histone modifications.
Science, 371, 2021
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6C23
 | | Cryo-EM structure of PRC2 bound to cofactors AEBP2 and JARID2 in the Compact Active State | | 分子名称: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH2, JARID2-substrate, ... | | 著者 | Kasinath, V, Faini, M, Poepsel, S, Reif, D, Feng, A, Stjepanovic, G, Aebersold, R, Nogales, E. | | 登録日 | 2018-01-05 | | 公開日 | 2018-01-24 | | 最終更新日 | 2019-12-18 | | 実験手法 | ELECTRON MICROSCOPY (3.9 Å) | | 主引用文献 | Structures of human PRC2 with its cofactors AEBP2 and JARID2.
Science, 359, 2018
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7KSO
 | | Cryo-EM structure of PRC2:EZH1-AEBP2-JARID2 | | 分子名称: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH1, Polycomb protein EED, ... | | 著者 | Grau, D.J, Armache, K.J. | | 登録日 | 2020-11-23 | | 公開日 | 2021-02-03 | | 最終更新日 | 2024-03-06 | | 実験手法 | ELECTRON MICROSCOPY (3.9 Å) | | 主引用文献 | Structures of monomeric and dimeric PRC2:EZH1 reveal flexible modules involved in chromatin compaction.
Nat Commun, 12, 2021
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5WG6
 | | Human Polycomb Repressive Complex 2 in complex with GSK126 inhibitor | | 分子名称: | 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3-methyl-6-[6-(piperazin-1-yl)pyridin-3-yl]-1H-indole-4-carboxamide, Histone-lysine N-methyltransferase EZH2,Polycomb protein SUZ12 (E.C.2.1.1.43) chimera, Polycomb protein EED, ... | | 著者 | Bratkowski, M.A, Liu, X. | | 登録日 | 2017-07-13 | | 公開日 | 2018-06-27 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.901 Å) | | 主引用文献 | An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
Sci Rep, 8, 2018
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7KSR
 | | PRC2:EZH1_A from a dimeric PRC2 bound to a nucleosome | | 分子名称: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH1, Polycomb protein EED, ... | | 著者 | Grau, D.J, Armache, K.J. | | 登録日 | 2020-11-24 | | 公開日 | 2021-02-03 | | 最終更新日 | 2024-03-06 | | 実験手法 | ELECTRON MICROSCOPY (4.1 Å) | | 主引用文献 | Structures of monomeric and dimeric PRC2:EZH1 reveal flexible modules involved in chromatin compaction.
Nat Commun, 12, 2021
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7AT8
 | | Histone H3 recognition by nucleosome-bound PRC2 subunit EZH2. | | 分子名称: | Histone H2A, Histone H2B 1.1, Histone H3.2, ... | | 著者 | Finogenova, K, Benda, C, Schaefer, I.B, Poepsel, S, Strauss, M, Mueller, J. | | 登録日 | 2020-10-29 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | ELECTRON MICROSCOPY (4.4 Å) | | 主引用文献 | Structural basis for PRC2 decoding of active histone methylation marks H3K36me2/3.
Elife, 9, 2020
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7KTP
 | | PRC2:EZH1_B from a dimeric PRC2 bound to a nucleosome | | 分子名称: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH1, Polycomb protein EED, ... | | 著者 | Grau, D.J, Armache, K.J. | | 登録日 | 2020-11-24 | | 公開日 | 2021-02-03 | | 最終更新日 | 2024-03-06 | | 実験手法 | ELECTRON MICROSCOPY (4.8 Å) | | 主引用文献 | Structures of monomeric and dimeric PRC2:EZH1 reveal flexible modules involved in chromatin compaction.
Nat Commun, 12, 2021
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