5V21
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5V3H
| Crystal structure of SMYD2 with SAM and EPZ033294 | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, GLYCEROL, ... | Authors: | Boriack-Sjodin, P.A. | Deposit date: | 2017-03-07 | Release date: | 2018-04-25 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.69 Å) | Cite: | Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation. Plos One, 13, 2018
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5V9J
| Crystal structure of catalytic domain of GLP with MS0105 | Descriptor: | CHLORIDE ION, DIMETHYL SULFOXIDE, Histone-lysine N-methyltransferase EHMT1, ... | Authors: | Dong, A, Zeng, H, Liu, J, Xiong, Y, Babault, N, Jin, J, Tempel, W, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Wu, H, Brown, P.J, Structural Genomics Consortium (SGC) | Deposit date: | 2017-03-23 | Release date: | 2018-03-21 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.74 Å) | Cite: | Crystal structure of catalytic domain of GLP with MS0105 to be published
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5VSF
| Structure of human GLP SET-domain (EHMT1) in complex with inhibitor 17 | Descriptor: | 1,4-DIETHYLENE DIOXIDE, GLYCEROL, Histone-lysine N-methyltransferase EHMT1, ... | Authors: | Babault, N, Xiong, Y, Liu, J, Jin, J. | Deposit date: | 2017-05-11 | Release date: | 2017-07-12 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Structure-activity relationship studies of G9a-like protein (GLP) inhibitors. Bioorg. Med. Chem., 25, 2017
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5VSE
| Structure of human G9a SET-domain (EHMT2) in complex with inhibitor 17: N~2~-cyclopentyl-6,7-dimethoxy-N~2~-methyl-N~4~-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine | Descriptor: | Histone-lysine N-methyltransferase EHMT2, N~2~-cyclopentyl-6,7-dimethoxy-N~2~-methyl-N~4~-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine, S-ADENOSYLMETHIONINE, ... | Authors: | Babault, N, Xiong, Y, Liu, J, Jin, J. | Deposit date: | 2017-05-11 | Release date: | 2017-07-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.6 Å) | Cite: | Structure-activity relationship studies of G9a-like protein (GLP) inhibitors. Bioorg. Med. Chem., 25, 2017
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5VSD
| Structure of human GLP SET-domain (EHMT1) in complex with inhibitor 13 | Descriptor: | 1,4-DIETHYLENE DIOXIDE, 6,7-dimethoxy-N~2~-methyl-N~4~-(1-methylpiperidin-4-yl)-N~2~-propylquinazoline-2,4-diamine, GLYCEROL, ... | Authors: | Babault, N, Xiong, Y, Liu, J, Jin, J. | Deposit date: | 2017-05-11 | Release date: | 2017-07-12 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Structure-activity relationship studies of G9a-like protein (GLP) inhibitors. Bioorg. Med. Chem., 25, 2017
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5TTG
| Crystal structure of catalytic domain of GLP with MS012 | Descriptor: | CHLORIDE ION, DIMETHYL SULFOXIDE, GLYCEROL, ... | Authors: | DONG, A, ZENG, H, LIU, J, XIONG, Y, BABAULT, N, JIN, J, TEMPEL, W, Bountra, C, Arrowsmith, C.H, Edwards, A.M, WU, H, BROWN, P.J, Structural Genomics Consortium (SGC) | Deposit date: | 2016-11-03 | Release date: | 2017-02-01 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.66 Å) | Cite: | Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. J. Med. Chem., 60, 2017
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5VSC
| Structure of human G9a SET-domain (EHMT2) in complex with inhibitor 13 | Descriptor: | 6,7-dimethoxy-N~2~-methyl-N~4~-(1-methylpiperidin-4-yl)-N~2~-propylquinazoline-2,4-diamine, Histone-lysine N-methyltransferase EHMT2, S-ADENOSYLMETHIONINE, ... | Authors: | Babault, N, Xiong, Y, Liu, J, Jin, J. | Deposit date: | 2017-05-11 | Release date: | 2017-07-12 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.4 Å) | Cite: | Structure-activity relationship studies of G9a-like protein (GLP) inhibitors. Bioorg. Med. Chem., 25, 2017
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5WCG
| SET and MYND Domain Containing protein 2 | Descriptor: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, DIMETHYL SULFOXIDE, N-lysine methyltransferase SMYD2, ... | Authors: | Dong, A, Zeng, H, Walker, J.R, Hutch, A, Seitova, A, Tatlock, J, Kumpf, R, Owen, A, Taylor, A, Casimiro-Garcia, A, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Brown, P.J, Wu, H, Structural Genomics Consortium (SGC) | Deposit date: | 2017-06-30 | Release date: | 2017-08-02 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.02 Å) | Cite: | The crystal structure of SMYD2 in complex with compound MTF003 to be published
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5V9I
| Crystal structure of catalytic domain of G9a with MS0105 | Descriptor: | GLYCEROL, Histone-lysine N-methyltransferase EHMT2, N~2~-cyclohexyl-N~4~-(1-ethylpiperidin-4-yl)-6,7-dimethoxy-N~2~-methylquinazoline-2,4-diamine, ... | Authors: | Dong, A, Zeng, H, Liu, J, Xiong, Y, Babault, N, Jin, J, Walker, J.R, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Wu, H, Brown, P.J, Structural Genomics Consortium (SGC) | Deposit date: | 2017-03-23 | Release date: | 2018-03-21 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.74 Å) | Cite: | Crystal structure of catalytic domain of G9a with MS0105 to be published
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5V37
| Crystal structure of SMYD3 with SAM and EPZ028862 | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, DIMETHYL SULFOXIDE, ... | Authors: | Boriack-Sjodin, P.A. | Deposit date: | 2017-03-06 | Release date: | 2018-03-07 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (1.42 Å) | Cite: | Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation. Plos One, 13, 2018
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5V22
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5UPD
| Methyltransferase domain of human Wolf-Hirschhorn Syndrome Candidate 1-Like protein 1 (WHSC1L1) | Descriptor: | Histone-lysine N-methyltransferase NSD3, S-ADENOSYLMETHIONINE, UNKNOWN ATOM OR ION, ... | Authors: | Tempel, W, Yu, W, Dong, A, Cerovina, T, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Brown, P.J, Wu, H, Structural Genomics Consortium (SGC) | Deposit date: | 2017-02-02 | Release date: | 2017-02-15 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Methyltransferase domain of human Wolf-Hirschhorn Syndrome Candidate 1-Like protein 1 (WHSC1L1) To Be Published
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7AT8
| Histone H3 recognition by nucleosome-bound PRC2 subunit EZH2. | Descriptor: | Histone H2A, Histone H2B 1.1, Histone H3.2, ... | Authors: | Finogenova, K, Benda, C, Schaefer, I.B, Poepsel, S, Strauss, M, Mueller, J. | Deposit date: | 2020-10-29 | Release date: | 2020-12-09 | Last modified: | 2024-05-01 | Method: | ELECTRON MICROSCOPY (4.4 Å) | Cite: | Structural basis for PRC2 decoding of active histone methylation marks H3K36me2/3. Elife, 9, 2020
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5M5G
| Crystal structure of the Chaetomium Thermophilum polycomb repressive complex 2 (PRC2) | Descriptor: | Fragment from molecular 2 (region containing putative polycomb protein Suz12), HISTONE H3 11-Mer peptide, Putative uncharacterized protein, ... | Authors: | Zhang, Y, Justin, N, Wilson, J, Gamblin, S. | Deposit date: | 2016-10-21 | Release date: | 2017-01-11 | Last modified: | 2019-10-16 | Method: | X-RAY DIFFRACTION (2.27 Å) | Cite: | Comment on "Structural basis of histone H3K27 trimethylation by an active polycomb repressive complex 2". Science, 354, 2016
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7YRD
| histone methyltransferase | Descriptor: | DNA (146-MER), Histone H2A.Z, Histone H2B 1.1, ... | Authors: | Li, H, Wang, W.Y. | Deposit date: | 2022-08-09 | Release date: | 2023-08-16 | Last modified: | 2023-12-13 | Method: | ELECTRON MICROSCOPY (3.2 Å) | Cite: | Structural insight into H4K20 methylation on H2A.Z-nucleosome by SUV420H1. Mol.Cell, 83, 2023
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7YRG
| histone methyltransferase | Descriptor: | DNA (146-MER), Histone H2A.Z, Histone H2B 1.1, ... | Authors: | Li, H, Wang, W.Y. | Deposit date: | 2022-08-09 | Release date: | 2023-12-13 | Method: | ELECTRON MICROSCOPY (4.2 Å) | Cite: | Structural insight into H4K20 methylation on H2A.Z-nucleosome by SUV420H1. Mol.Cell, 83, 2023
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8JHF
| Native SUV420H1 bound to 167-bp nucleosome | Descriptor: | DNA (160-MER), Histone H2A.Z, Histone H2B type 1-K, ... | Authors: | Lin, F, Li, W. | Deposit date: | 2023-05-23 | Release date: | 2023-11-15 | Last modified: | 2023-12-20 | Method: | ELECTRON MICROSCOPY (3.68 Å) | Cite: | Structural basis of nucleosomal H4K20 recognition and methylation by SUV420H1 methyltransferase. Cell Discov, 9, 2023
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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 | Descriptor: | 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, ... | Authors: | Gajiwala, K.S, Brooun, A, Liu, W, Deng, Y, Stewart, A.E. | Deposit date: | 2017-09-25 | Release date: | 2017-12-27 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.81 Å) | Cite: | 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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8JHG
| Native SUV420H1 bound to 167-bp nucleosome | Descriptor: | DNA (160-MER), Histone H2A type 1-B/E, Histone H2B type 1-K, ... | Authors: | Lin, F, Li, W. | Deposit date: | 2023-05-23 | Release date: | 2023-11-22 | Last modified: | 2023-12-20 | Method: | ELECTRON MICROSCOPY (3.58 Å) | Cite: | Structural basis of nucleosomal H4K20 recognition and methylation by SUV420H1 methyltransferase. Cell Discov, 9, 2023
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5BJS
| Apo ctPRC2 in an autoinhibited state | Descriptor: | Histone-lysine N-methyltransferase EZH2, Polycomb protein SUZ12, Polycomb Protein EED, ... | Authors: | Bratkowski, M.A, Liu, X. | Deposit date: | 2016-10-22 | Release date: | 2017-06-14 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.189 Å) | Cite: | Polycomb repressive complex 2 in an autoinhibited state. J. Biol. Chem., 292, 2017
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8FYH
| G4 RNA-mediated PRC2 dimer | Descriptor: | G4 RNA, Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH2, ... | Authors: | Song, J, Kasinath, V. | Deposit date: | 2023-01-26 | Release date: | 2023-10-04 | Method: | ELECTRON MICROSCOPY (3.4 Å) | Cite: | Structural basis for inactivation of PRC2 by G-quadruplex RNA. Science, 381, 2023
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7KSO
| Cryo-EM structure of PRC2:EZH1-AEBP2-JARID2 | Descriptor: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH1, Polycomb protein EED, ... | Authors: | Grau, D.J, Armache, K.J. | Deposit date: | 2020-11-23 | Release date: | 2021-02-03 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (3.9 Å) | Cite: | Structures of monomeric and dimeric PRC2:EZH1 reveal flexible modules involved in chromatin compaction. Nat Commun, 12, 2021
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7KSR
| PRC2:EZH1_A from a dimeric PRC2 bound to a nucleosome | Descriptor: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH1, Polycomb protein EED, ... | Authors: | Grau, D.J, Armache, K.J. | Deposit date: | 2020-11-24 | Release date: | 2021-02-03 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (4.1 Å) | Cite: | Structures of monomeric and dimeric PRC2:EZH1 reveal flexible modules involved in chromatin compaction. Nat Commun, 12, 2021
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7KTP
| PRC2:EZH1_B from a dimeric PRC2 bound to a nucleosome | Descriptor: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH1, Polycomb protein EED, ... | Authors: | Grau, D.J, Armache, K.J. | Deposit date: | 2020-11-24 | Release date: | 2021-02-03 | Last modified: | 2024-03-06 | Method: | ELECTRON MICROSCOPY (4.8 Å) | Cite: | Structures of monomeric and dimeric PRC2:EZH1 reveal flexible modules involved in chromatin compaction. Nat Commun, 12, 2021
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