3HNA
| Crystal structure of catalytic domain of human euchromatic histone methyltransferase 1 in complex with SAH and mono-Methylated H3K9 Peptide | Descriptor: | Histone-lysine N-methyltransferase, H3 lysine-9 specific 5, Mono-Methylated H3K9 Peptide, ... | Authors: | Min, J, Wu, H, Loppnau, P, Wleigelt, J, Sundstrom, M, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Plotnikov, A.N, Structural Genomics Consortium (SGC) | Deposit date: | 2009-05-30 | Release date: | 2009-06-09 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Structural biology of human H3K9 methyltransferases Plos One, 5, 2010
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2RFI
| Crystal structure of catalytic domain of human euchromatic histone methyltransferase 1 in complex with SAH and dimethylated H3K9 peptide | Descriptor: | Histone H3, Histone-lysine N-methyltransferase, H3 lysine-9 specific 5, ... | Authors: | Min, J, Wu, H, Loppnau, P, Weigelt, J, Sundstrom, M, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Plotnikov, A.N, Structural Genomics Consortium (SGC) | Deposit date: | 2007-09-30 | Release date: | 2007-10-23 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (1.59 Å) | Cite: | Structural biology of human H3K9 methyltransferases Plos One, 5, 2010
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6MBO
| GLP Methyltransferase with Inhibitor EML741-P212121 Crystal Form | Descriptor: | 1,2-ETHANEDIOL, 2-cyclohexyl-7-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-8-[3-(pyrrolidin-1-yl)propoxy]-3H-1,4-benzodiazepin-5-amine, Histone-lysine N-methyltransferase EHMT1, ... | Authors: | Horton, J.R, Cheng, X. | Deposit date: | 2018-08-30 | Release date: | 2019-02-27 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.591 Å) | Cite: | Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. J. Med. Chem., 62, 2019
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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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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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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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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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4I51
| Methyltransferase domain of HUMAN EUCHROMATIC HISTONE METHYLTRANSFERASE 1, mutant Y1211A | Descriptor: | GLYCEROL, H3K9 NE-ALLYL PEPTIDE, Histone-lysine N-methyltransferase EHMT1, ... | Authors: | Dong, A, Zeng, H, Walker, J.R, Islam, K, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Lou, M, Min, J, Wu, H, Structural Genomics Consortium (SGC) | Deposit date: | 2012-11-28 | Release date: | 2012-12-19 | Last modified: | 2023-12-06 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Defining efficient enzyme-cofactor pairs for bioorthogonal profiling of protein methylation. Proc.Natl.Acad.Sci.USA, 110, 2013
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6MBP
| GLP Methyltransferase with Inhibitor EML741- P3121 Crystal Form | Descriptor: | 1,2-ETHANEDIOL, 2-cyclohexyl-7-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-8-[3-(pyrrolidin-1-yl)propoxy]-3H-1,4-benzodiazepin-5-amine, Histone-lysine N-methyltransferase EHMT1, ... | Authors: | Horton, J.R, Cheng, X. | Deposit date: | 2018-08-30 | Release date: | 2019-02-27 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.947 Å) | Cite: | Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. J. Med. Chem., 62, 2019
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5TUZ
| Structure of human GLP SET-domain (EHMT1) in complex with inhibitor MS0124 | Descriptor: | 1,2-ETHANEDIOL, 6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(morpholin-4-yl)quinazolin-4-amine, Histone-lysine N-methyltransferase EHMT1, ... | Authors: | Babault, N, Xiong, Y, Liu, J, Jin, J. | Deposit date: | 2016-11-07 | Release date: | 2017-02-22 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. J. Med. Chem., 60, 2017
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2IGQ
| Human euchromatic histone methyltransferase 1 | Descriptor: | S-ADENOSYL-L-HOMOCYSTEINE, ZINC ION, euchromatic histone methyltransferase 1 | Authors: | Min, J, Wu, H, Antoshenko, T, Loppnau, P, Weigelt, J, Sundstrom, M, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Plotnikov, A.N, Structural Genomics Consortium (SGC) | Deposit date: | 2006-09-23 | Release date: | 2006-10-24 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Structural biology of human H3K9 methyltransferases Plos One, 5, 2010
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3MO5
| Human G9a-like (GLP, also known as EHMT1) in complex with inhibitor E72 | Descriptor: | 7-[(5-aminopentyl)oxy]-N~4~-[1-(5-aminopentyl)piperidin-4-yl]-N~2~-[3-(dimethylamino)propyl]-6-methoxyquinazoline-2,4-diamine, Histone-lysine N-methyltransferase, H3 lysine-9 specific 5, ... | Authors: | Chang, Y, Horton, J.R, Cheng, X. | Deposit date: | 2010-04-22 | Release date: | 2010-06-30 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.14 Å) | Cite: | Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferases. J.Mol.Biol., 400, 2010
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6BY9
| Crystal structure of EHMT1 | Descriptor: | Histone-lysine N-methyltransferase EHMT1, UNKNOWN ATOM OR ION | Authors: | Dong, A, Wei, Y, Li, A, Tempel, W, Han, S, Sunnerhagen, M, Penn, L, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Tong, Y, Structural Genomics Consortium (SGC) | Deposit date: | 2017-12-20 | Release date: | 2018-01-31 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Crystal structure of EHMT1 to be published
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3SWC
| GLP (G9a-like protein) SET domain in complex with Dnmt3aK44me2 peptide | Descriptor: | DNA (cytosine-5)-methyltransferase 3A, Histone-lysine N-methyltransferase EHMT1, S-ADENOSYL-L-HOMOCYSTEINE, ... | Authors: | Chang, Y, Horton, J.R, Zhang, X, Cheng, X. | Deposit date: | 2011-07-13 | Release date: | 2011-11-30 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (2.332 Å) | Cite: | MPP8 mediates the interactions between DNA methyltransferase Dnmt3a and H3K9 methyltransferase GLP/G9a. Nat Commun, 2, 2011
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3FPD
| G9a-like protein lysine methyltransferase inhibition by BIX-01294 | Descriptor: | Histone-lysine N-methyltransferase, H3 lysine-9 specific 5, N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine, ... | Authors: | Chang, Y, Zhang, X, Horton, J.R, Cheng, X. | Deposit date: | 2009-01-05 | Release date: | 2009-02-17 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat.Struct.Mol.Biol., 16, 2009
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3MO2
| human G9a-like (GLP, also known as EHMT1) in complex with inhibitor E67 | Descriptor: | 7-[(5-aminopentyl)oxy]-N~4~-(1-benzylpiperidin-4-yl)-N~2~-[3-(dimethylamino)propyl]-6-methoxyquinazoline-2,4-diamine, Histone-lysine N-methyltransferase, H3 lysine-9 specific 5, ... | Authors: | Chang, Y, Horton, J.R, Cheng, X. | Deposit date: | 2010-04-22 | Release date: | 2010-06-30 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.49 Å) | Cite: | Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferases. J.Mol.Biol., 400, 2010
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3MO0
| Human G9a-like (GLP, also known as EHMT1) in complex with inhibitor E11 | Descriptor: | 1,2-ETHANEDIOL, Histone-lysine N-methyltransferase, H3 lysine-9 specific 5, ... | Authors: | Chang, Y, Horton, J.R, Cheng, X. | Deposit date: | 2010-04-22 | Release date: | 2010-06-30 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.78 Å) | Cite: | Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferases. J.Mol.Biol., 400, 2010
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7T7M
| Structure of human GLP SET-domain (EHMT1) in complex with covalent inhibitor (Compound 1) | Descriptor: | Histone-lysine N-methyltransferase EHMT1, N-(6-methoxy-4-{[1-(propan-2-yl)piperidin-4-yl]amino}-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-2-yl)prop-2-enamide, N-(6-methoxy-4-{[1-(propan-2-yl)piperidin-4-yl]amino}-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-2-yl)propanamide, ... | Authors: | Park, K.-S, Kumar, P. | Deposit date: | 2021-12-15 | Release date: | 2022-07-06 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.85 Å) | Cite: | Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. J.Med.Chem., 65, 2022
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3B95
| EuHMT1 (Glp) Ankyrin Repeat Domain (Structure 2) | Descriptor: | Euchromatic histone-lysine N-methyltransferase 1, Histone H3 N-terminal Peptide, SULFATE ION | Authors: | Collins, R.E, Horton, J.R, Cheng, X. | Deposit date: | 2007-11-02 | Release date: | 2008-02-12 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.99 Å) | Cite: | The ankyrin repeats of G9a and GLP histone methyltransferases are mono- and dimethyllysine binding modules. Nat.Struct.Mol.Biol., 15, 2008
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3B7B
| EuHMT1 (Glp) Ankyrin Repeat Domain (Structure 1) | Descriptor: | Euchromatic histone-lysine N-methyltransferase 1, SULFATE ION | Authors: | Collins, R.E, Horton, J.R, Cheng, X. | Deposit date: | 2007-10-30 | Release date: | 2008-02-12 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.99 Å) | Cite: | The ankyrin repeats of G9a and GLP histone methyltransferases are mono- and dimethyllysine binding modules Nat.Struct.Mol.Biol., 15, 2008
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3SW9
| GLP (G9a-like protein) SET domain in complex with Dnmt3aK44me0 peptide | Descriptor: | DNA (cytosine-5)-methyltransferase 3A, Histone-lysine N-methyltransferase EHMT1, SINEFUNGIN, ... | Authors: | Chang, Y, Horton, J.R, Zhang, X, Cheng, X. | Deposit date: | 2011-07-13 | Release date: | 2011-12-07 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (3.05 Å) | Cite: | MPP8 mediates the interactions between DNA methyltransferase Dnmt3a and H3K9 methyltransferase GLP/G9a. Nat Commun, 2, 2011
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8XPT
| The Crystal Structure of EHMT1 from Biortus. | Descriptor: | Histone-lysine N-methyltransferase EHMT1, S-ADENOSYL-L-HOMOCYSTEINE, SULFATE ION, ... | Authors: | Wang, F, Cheng, W, Yuan, Z, Lin, D, Bao, C. | Deposit date: | 2024-01-04 | Release date: | 2024-01-24 | Method: | X-RAY DIFFRACTION (3.35 Å) | Cite: | The Crystal Structure of EHMT1 from Biortus. To Be Published
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