4MI0
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HUMAN ENHANCER OF ZESTE (DROSOPHILA) HOMOLOG 2(EZH2)
Descriptor:Histone-lysine N-methyltransferase EZH2, ZINC ION, UNKNOWN ATOM OR ION
Authors:Dong, A., Zeng, H., He, H., Wernimont, A., Bountra, C., Arrowsmith, C.H., Edwards, A.M., Brown, P.J., Wu, H., Structural Genomics Consortium (SGC)
Deposit date:2013-08-30
Release date:2013-09-25
Last modified:2017-11-15
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structure of the catalytic domain of EZH2 reveals conformational plasticity in cofactor and substrate binding sites and explains oncogenic mutations.
Plos One, 8, 2013
4MI5
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CRYSTAL STRUCTURE OF THE EZH2 SET DOMAIN
Descriptor:Histone-lysine N-methyltransferase EZH2, SULFATE ION, ZINC ION
Authors:Antonysamy, S., Condon, B., Druzina, Z., Bonanno, J., Gheyi, T., Macewan, I., Zhang, A., Ashok, S., Russell, M., Luz, J.G.
Deposit date:2013-08-30
Release date:2014-01-08
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structural Context of Disease-Associated Mutations and Putative Mechanism of Autoinhibition Revealed by X-Ray Crystallographic Analysis of the EZH2-SET Domain.
Plos One, 8, 2013
6U4Y
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CRYSTAL STRUCTURE OF AN EZH2-EED COMPLEX IN AN OLIGOMERIC STATE
Descriptor:Histone-lysine N-methyltransferase EZH2, Polycomb protein EED
Authors:Jiao, L., Liu, X.
Deposit date:2019-08-26
Release date:2020-07-08
Last modified:2020-08-12
Method:X-RAY DIFFRACTION (2.91 Å)
Cite:A partially disordered region connects gene repression and activation functions of EZH2.
Proc.Natl.Acad.Sci.USA, 117, 2020
5LS6
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STRUCTURE OF HUMAN POLYCOMB REPRESSIVE COMPLEX 2 (PRC2) WITH INHIBITOR
Descriptor:Histone-lysine N-methyltransferase EZH2,Histone-lysine N-methyltransferase EZH2,Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, Polycomb protein SUZ12, ...
Authors:Zhang, Y., Justin, N., Chen, S., Wilson, J., Gamblin, S.
Deposit date:2016-08-22
Release date:2017-02-22
Last modified:2019-07-10
Method:X-RAY DIFFRACTION (3.47 Å)
Cite: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
5WG6
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HUMAN POLYCOMB REPRESSIVE COMPLEX 2 IN COMPLEX WITH GSK126 INHIBITOR
Descriptor:Histone-lysine N-methyltransferase EZH2,Polycomb protein SUZ12 (E.C.2.1.1.43) chimera, Polycomb protein EED, ZINC ION, ...
Authors:Bratkowski, M.A., Liu, X.
Deposit date:2017-07-13
Release date:2018-06-27
Last modified:2020-01-08
Method:X-RAY DIFFRACTION (3.901 Å)
Cite:An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
Sci Rep, 8, 2018
2QXV
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STRUCTURAL BASIS OF EZH2 RECOGNITION BY EED
Descriptor:Embryonic ectoderm development, Enhancer of zeste homolog 2
Authors:Han, Z.
Deposit date:2007-08-13
Release date:2007-08-28
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.82 Å)
Cite:Structural basis of EZH2 recognition by EED
Structure, 15, 2007
5WUK
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CRYSTAL STRUCTURE OF EED [G255D] IN COMPLEX WITH EZH2 PEPTIDE AND EED226 COMPOUND
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, GLYCEROL, ...
Authors:Chen, Z.
Deposit date:2016-12-19
Release date:2017-05-03
Method:X-RAY DIFFRACTION (2.03 Å)
Cite:Split luciferase-based biosensors for characterizing EED binders
Anal. Biochem., 522, 2017
5WF7
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CHAETOMIUM THERMOPHILUM POLYCOMB REPRESSIVE COMPLEX 2 BOUND TO GSK126
Descriptor:Polycomb Protein EED, Histone-lysine-N-methyltransferase EZH2, Polycomb protein SUZ12 chimera, ...
Authors:Bratkowski, M.A., Liu, X.
Deposit date:2017-07-11
Release date:2018-06-27
Last modified:2020-01-08
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
Sci Rep, 8, 2018
5WFC
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HUMANIZED MUTANT OF THE CHAETOMIUM THERMOPHILUM POLYCOMB REPRESSIVE COMPLEX 2 BOUND TO THE INHIBITOR GSK343
Descriptor:Polycomb Protein EED, Histone-lysine-N-methyltransferase EZH2, Polycomb protein SUZ12 chimera, ...
Authors:Bratkowski, M.A., Liu, X.
Deposit date:2017-07-11
Release date:2018-06-27
Last modified:2020-01-08
Method:X-RAY DIFFRACTION (2.282 Å)
Cite:An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
Sci Rep, 8, 2018
5WFD
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HUMANIZED MUTANT OF THE CHAETOMIUM THERMOPHILUM POLYCOMB REPRESSIVE COMPLEX 2 BOUND TO THE INHIBITOR GSK126
Descriptor:Polycomb Protein EED, Histone-lysine-N-methyltransferase EZH2, Polycomb protein SUZ12 chimera, ...
Authors:Bratkowski, M.A., Liu, X.
Deposit date:2017-07-11
Release date:2018-06-27
Last modified:2020-01-08
Method:X-RAY DIFFRACTION (2.654 Å)
Cite:An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
Sci Rep, 8, 2018
5IJ7
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STRUCTURE OF HS/ACPRC2 IN COMPLEX WITH A PYRIDONE INHIBITOR
Descriptor:Enhancer of Zeste Homolog 2 (EZH2),Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, Polycomb protein SUZ12, ...
Authors:Gajiwala, K.S., Brooun, A., Deng, Y.-L., Liu, W.
Deposit date:2016-03-01
Release date:2016-05-04
Last modified:2017-11-22
Method:X-RAY DIFFRACTION (2.62 Å)
Cite:Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.
Nat Commun, 7, 2016
5IJ8
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STRUCTURE OF THE PRIMARY ONCOGENIC MUTANT Y641N HS/ACPRC2 IN COMPLEX WITH A PYRIDONE INHIBITOR
Descriptor:Enhancer of Zeste Homolog 2 (EZH2),Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, Polycomb protein SUZ12, ...
Authors:Gajiwala, K.S., Brooun, A., Deng, Y.-L., Liu, W.
Deposit date:2016-03-01
Release date:2016-05-04
Last modified:2017-11-22
Method:X-RAY DIFFRACTION (2.99 Å)
Cite:Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.
Nat Commun, 7, 2016
5HYN
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STRUCTURE OF HUMAN POLYCOMB REPRESSIVE COMPLEX 2 (PRC2) WITH ONCOGENIC HISTONE H3K27M PEPTIDE
Descriptor:Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, Polycomb protein SUZ12, ...
Authors:Zhang, Y., Justin, N., Wilson, J.R., Gamblin, S.J.
Deposit date:2016-02-01
Release date:2016-05-11
Method:X-RAY DIFFRACTION (2.95 Å)
Cite:Structural basis of oncogenic histone H3K27M inhibition of human polycomb repressive complex 2.
Nat Commun, 7, 2016
6C23
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CRYO-EM STRUCTURE OF PRC2 BOUND TO COFACTORS AEBP2 AND JARID2 IN THE COMPACT ACTIVE STATE
Descriptor:Polycomb protein SUZ12, Protein Jumonji, Histone-lysine N-methyltransferase EZH2, ...
Authors:Kasinath, V., Faini, M., Poepsel, S., Reif, D., Feng, A., Stjepanovic, G., Aebersold, R., Nogales, E.
Deposit date:2018-01-05
Release date:2018-01-24
Last modified:2019-12-18
Method:ELECTRON MICROSCOPY (3.9 Å)
Cite:Structures of human PRC2 with its cofactors AEBP2 and JARID2.
Science, 359, 2018
6C24
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CRYO-EM STRUCTURE OF PRC2 BOUND TO COFACTORS AEBP2 AND JARID2 IN THE EXTENDED ACTIVE STATE
Descriptor:Polycomb protein SUZ12, Protein Jumonji, Histone-lysine N-methyltransferase EZH2, ...
Authors:Kasinath, V., Faini, M., Poepsel, S., Reif, D., Feng, A., Stjepanovic, G., Aebersold, R., Nogales, E.
Deposit date:2018-01-06
Release date:2018-01-24
Last modified:2019-12-18
Method:ELECTRON MICROSCOPY (3.5 Å)
Cite:Structures of human PRC2 with its cofactors AEBP2 and JARID2.
Science, 359, 2018
5GSA
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EED IN COMPLEX WITH AN ALLOSTERIC PRC2 INHIBITOR
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, N-(furan-2-ylmethyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine
Authors:Zhao, K., Zhao, M., Luo, X., Zhang, H.
Deposit date:2016-08-15
Release date:2017-02-01
Last modified:2017-04-05
Method:X-RAY DIFFRACTION (2.49 Å)
Cite:An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of
Nat. Chem. Biol., 13, 2017
5H14
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EED IN COMPLEX WITH AN ALLOSTERIC PRC2 INHIBITOR EED666
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, GLYCEROL, ...
Authors:Zhao, K., Zhao, M., Luo, X., Zhang, H.
Deposit date:2016-10-08
Release date:2017-01-25
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
5H15
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EED IN COMPLEX WITH PRC2 ALLOSTERIC INHIBITOR EED709
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, (3R,4S)-1-[(2-methoxyphenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine
Authors:Zhao, K., Zhao, M., Luo, X., Zhang, H.
Deposit date:2016-10-08
Release date:2017-01-25
Method:X-RAY DIFFRACTION (2.27 Å)
Cite:Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
5H17
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EED IN COMPLEX WITH PRC2 ALLOSTERIC INHIBITOR EED210
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, (3R,4aS,10aS)-6-methoxy-3-[(3-methoxyphenyl)methyl]-1-methyl-3,4,4a,5,10,10a-hexahydro-2H-benzo[g]quinoline
Authors:Zhao, K., Zhao, M., Luo, X., Zhang, H.
Deposit date:2016-10-08
Release date:2017-01-25
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
5H19
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EED IN COMPLEX WITH PRC2 ALLOSTERIC INHIBITOR EED162
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, 5-(furan-2-ylmethylamino)-9-(phenylmethyl)-8,10-dihydro-7H-[1,2,4]triazolo[3,4-a][2,7]naphthyridine-6-carbonitrile
Authors:Zhao, K., Zhao, M., Luo, X., Zhang, H.
Deposit date:2016-10-08
Release date:2017-01-25
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
PLoS ONE, 12, 2017
5H24
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EED IN COMPLEX WITH PRC2 ALLOSTERIC INHIBITOR COMPOUND 8
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, 5-(furan-2-ylmethylamino)-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrile
Authors:Zhao, K., Zhao, M., Luo, X., Zhang, H.
Deposit date:2016-10-14
Release date:2017-01-25
Last modified:2017-04-05
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
J. Med. Chem., 60, 2017
5H25
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EED IN COMPLEX WITH PRC2 ALLOSTERIC INHIBITOR COMPOUND 11
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, 5-(2-fluorophenyl)-2,3-dihydroimidazo[2,1-a]isoquinoline
Authors:Zhao, K., Zhao, M., Luo, X., Zhang, H.
Deposit date:2016-10-14
Release date:2017-01-25
Last modified:2017-04-05
Method:X-RAY DIFFRACTION (2.88 Å)
Cite:Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
J. Med. Chem., 60, 2017
5U5T
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CRYSTAL STRUCTURE OF EED IN COMPLEX WITH H3K27ME3 PEPTIDE AND 3-(BENZO[D][1,3]DIOXOL-4-YLMETHYL)PIPERIDINE-1-CARBOXIMIDAMIDE
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, (3R)-3-[(2H-1,3-benzodioxol-4-yl)methyl]piperidine-1-carboximidamide, ...
Authors:Bussiere, D., Shu, W.
Deposit date:2016-12-07
Release date:2017-01-11
Last modified:2017-09-27
Method:X-RAY DIFFRACTION (1.6 Å)
Cite:Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
J. Med. Chem., 60, 2017
5U62
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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
Descriptor:Polycomb protein EED, Histone-lysine N-methyltransferase EZH2, GLYCEROL, ...
Authors:Bussiere, D., Shu, W.
Deposit date:2016-12-07
Release date:2017-01-11
Last modified:2017-09-27
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
J. Med. Chem., 60, 2017
5VK3
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APO CTPRC2 WITH E840A AND K852D MUTATIONS IN EZH2
Descriptor:Polycomb Protein EED, Histone-lysine N-methyltransferase EZH2,Polycomb protein SUZ12, ZINC ION
Authors:Bratkowski, M.A., Liu, X.
Deposit date:2017-04-20
Release date:2017-06-14
Last modified:2020-01-01
Method:X-RAY DIFFRACTION (2.114 Å)
Cite:Polycomb repressive complex 2 in an autoinhibited state.
J. Biol. Chem., 292, 2017
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171916
PDB entries from 2020-12-02