5F5E
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5HT6
| Crystal structure of the SET domain of the human MLL5 methyltransferase | Descriptor: | Histone-lysine N-methyltransferase 2E | Authors: | le Maire, A, Mas-y-Mas, S, Dumas, C, Lebedev, A. | Deposit date: | 2016-01-26 | Release date: | 2016-11-16 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.093 Å) | Cite: | The Human Mixed Lineage Leukemia 5 (MLL5), a Sequentially and Structurally Divergent SET Domain-Containing Protein with No Intrinsic Catalytic Activity. Plos One, 11, 2016
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5H6Z
| Crystal structure of Set7, a novel histone methyltransferase in Schizossacharomyces pombe | Descriptor: | AMMONIUM ION, DI(HYDROXYETHYL)ETHER, SET domain-containing protein 7, ... | Authors: | Mevius, D.E.H.F, Shen, Y, Morishita, M, Carrozzini, B, Caliandro, R, di Luccio, E. | Deposit date: | 2016-11-15 | Release date: | 2017-11-22 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Set7 Is a H3K37 Methyltransferase in Schizosaccharomyces pombe and Is Required for Proper Gametogenesis. Structure, 27, 2019
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6U9K
| MLL1 SET N3861I/Q3867L bound to inhibitor 18 (TC-5153) | Descriptor: | 5'-([(3S)-3-amino-3-carboxypropyl]{[1-(3,3-diphenylpropyl)azetidin-3-yl]methyl}amino)-5'-deoxyadenosine, GLYCEROL, Histone-lysine N-methyltransferase, ... | Authors: | Petrunak, E.M, Stuckey, J.A. | Deposit date: | 2019-09-09 | Release date: | 2020-07-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Discovery of Potent Small-Molecule Inhibitors of MLL Methyltransferase. Acs Med.Chem.Lett., 11, 2020
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6U9N
| MLL1 SET N3861I/Q3867L bound to inhibitor 14 (TC-5139) | Descriptor: | 5'-{[(3S)-3-amino-3-carboxypropyl]({1-[(4-chlorophenyl)methyl]azetidin-3-yl}methyl)amino}-5'-deoxyadenosine, Histone-lysine N-methyltransferase, ZINC ION | Authors: | Petrunak, E.M, Stuckey, J.A. | Deposit date: | 2019-09-09 | Release date: | 2020-07-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Discovery of Potent Small-Molecule Inhibitors of MLL Methyltransferase. Acs Med.Chem.Lett., 11, 2020
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6U9R
| MLL1 SET N3861I/Q3867L bound to inhibitor 12 (TC-5140) | Descriptor: | 5'-{[(3S)-3-amino-3-carboxypropyl]({1-[(3-chlorophenyl)methyl]azetidin-3-yl}methyl)amino}-5'-deoxyadenosine, Histone-lysine N-methyltransferase, ZINC ION | Authors: | Petrunak, E.M, Stuckey, J.A. | Deposit date: | 2019-09-09 | Release date: | 2020-07-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Discovery of Potent Small-Molecule Inhibitors of MLL Methyltransferase. Acs Med.Chem.Lett., 11, 2020
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6U9M
| MLL1 SET N3861I/Q3867L bound to inhibitor 16 (TC-5109) | Descriptor: | 5'-{[(3S)-3-amino-3-carboxypropyl]({1-[(thiophen-2-yl)methyl]azetidin-3-yl}methyl)amino}-5'-deoxyadenosine, GLYCEROL, Histone-lysine N-methyltransferase, ... | Authors: | Petrunak, E.M, Stuckey, J.A. | Deposit date: | 2019-09-09 | Release date: | 2020-07-01 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.05 Å) | Cite: | Discovery of Potent Small-Molecule Inhibitors of MLL Methyltransferase. Acs Med.Chem.Lett., 11, 2020
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6BOZ
| Structure of human SETD8 in complex with covalent inhibitor MS4138 | Descriptor: | 1,2-ETHANEDIOL, N-(3-{[7-(2-aminoethoxy)-6-methoxy-2-(pyrrolidin-1-yl)quinazolin-4-yl]amino}propyl)prop-2-enamide, N-lysine methyltransferase KMT5A | Authors: | Babault, N, Anqi, M, Jin, J. | Deposit date: | 2017-11-21 | Release date: | 2019-05-01 | Last modified: | 2019-12-04 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | The dynamic conformational landscape of the protein methyltransferase SETD8. Elife, 8, 2019
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3RQ4
| Crystal structure of suppressor of variegation 4-20 homolog 2 | Descriptor: | 1,2-ETHANEDIOL, Histone-lysine N-methyltransferase SUV420H2, S-ADENOSYLMETHIONINE, ... | Authors: | Dong, A, Zeng, H, Tempel, W, Loppnau, P, Bountra, C, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Min, J, Wu, H, Structural Genomics Consortium (SGC) | Deposit date: | 2011-04-27 | Release date: | 2011-06-01 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Crystal structures of the human histone H4K20 methyltransferases SUV420H1 and SUV420H2. Febs Lett., 587, 2013
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3KMT
| Crystal structure of vSET/SAH/H3 ternary complex | Descriptor: | A612L protein, Histone H3, S-ADENOSYL-L-HOMOCYSTEINE | Authors: | Wei, H, Zhou, M.M. | Deposit date: | 2009-11-11 | Release date: | 2010-11-10 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.78 Å) | Cite: | Dimerization of a viral SET protein endows its function. Proc.Natl.Acad.Sci.USA, 107, 2010
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3KMJ
| Crystal structure of vSET under condition B | Descriptor: | A612L protein, SULFATE ION | Authors: | Wei, H, Zhou, M.M. | Deposit date: | 2009-11-10 | Release date: | 2010-11-10 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Dimerization of a viral SET protein endows its function. Proc.Natl.Acad.Sci.USA, 107, 2010
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3KMA
| Crystal Structure of vSET under Condition A | Descriptor: | A612L protein, CHLORIDE ION, GLYCEROL, ... | Authors: | Wei, H, Zhou, M.M. | Deposit date: | 2009-11-10 | Release date: | 2010-11-10 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.6 Å) | Cite: | Dimerization of a viral SET protein endows its function. Proc.Natl.Acad.Sci.USA, 107, 2010
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5T5G
| human SETD8 in complex with MS2177 | Descriptor: | 7-(2-aminoethoxy)-6-methoxy-2-(pyrrolidin-1-yl)-N-[5-(pyrrolidin-1-yl)pentyl]quinazolin-4-amine, N-lysine methyltransferase KMT5A, UNKNOWN ATOM OR ION | Authors: | Yu, W, Tempel, W, Babault, N, Ma, A, Butler, K.V, Jin, J, Arrowsmith, C.H, Bountra, C, Edwards, A.M, Brown, P.J, Structural Genomics Consortium (SGC) | Deposit date: | 2016-08-30 | Release date: | 2016-09-28 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase. J. Med. Chem., 59, 2016
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5VA6
| CRYSTAL STRUCTURE OF ATXR5 IN COMPLEX WITH HISTONE H3.1 MONO-METHYLATED ON R26 | Descriptor: | Histone H3.1, Probable Histone-lysine N-methyltransferase ATXR5, S-ADENOSYL-L-HOMOCYSTEINE | Authors: | Bergamin, E, Sarvan, S, Malette, J, Eram, M, Yeung, S, Mongeon, V, Joshi, M, Brunzelle, J.S, Michaels, S.D, Blais, A, Vedadi, M, Couture, J.-F. | Deposit date: | 2017-03-24 | Release date: | 2017-04-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Molecular basis for the methylation specificity of ATXR5 for histone H3. Nucleic Acids Res., 45, 2017
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5V2N
| Crystal Structure of APO Human SETD8 | Descriptor: | 1,2-ETHANEDIOL, N-lysine methyltransferase KMT5A | Authors: | Skene, R.J. | Deposit date: | 2017-03-05 | Release date: | 2018-03-07 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | The dynamic conformational landscape of the protein methyltransferase SETD8. Elife, 8, 2019
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5VAH
| Crystal structure of ATXR5 SET domain in complex with histone H3 di-methylated on R26 | Descriptor: | Histone H3.2, Probable Histone-lysine N-methyltransferase ATXR5, S-ADENOSYL-L-HOMOCYSTEINE | Authors: | Bergamin, E, Sarvan, S, Malette, J, Eram, M, Yeung, S, Mongeon, V, Joshi, M, Brunzelle, J.S, Michaels, S.D, Blais, A, Vedadi, M, Couture, J.-F. | Deposit date: | 2017-03-26 | Release date: | 2017-04-05 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Molecular basis for the methylation specificity of ATXR5 for histone H3. Nucleic Acids Res., 45, 2017
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5TEG
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5VBC
| Crystal structure of ATXR5 in complex with histone H3.1 | Descriptor: | DIMETHYL SULFOXIDE, Histone H3.1 peptide, Probable Histone-lysine N-methyltransferase ATXR5, ... | Authors: | Couture, J.-F, Bergamin, E. | Deposit date: | 2017-03-29 | Release date: | 2017-04-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Molecular basis for the methylation specificity of ATXR5 for histone H3. Nucleic Acids Res., 45, 2017
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5TH7
| Complex of SETD8 with MS453 | Descriptor: | 1,2-ETHANEDIOL, N-(3-{[6,7-dimethoxy-2-(pyrrolidin-1-yl)quinazolin-4-yl]amino}propyl)propanamide, N-lysine methyltransferase KMT5A, ... | Authors: | Yu, W, Tempel, W, Babault, N, Ma, A, Butler, K.V, Jin, J, Arrowsmith, C.H, Bountra, C, Edwards, A.M, Brown, P.J, Structural Genomics Consortium (SGC) | Deposit date: | 2016-09-29 | Release date: | 2016-11-09 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase. J. Med. Chem., 59, 2016
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5W1Y
| SETD8 in complex with a covalent inhibitor | Descriptor: | 2-(4-methylpiperazin-1-yl)-3-(phenylsulfanyl)naphthalene-1,4-dione, N-lysine methyltransferase KMT5A, UNKNOWN ATOM OR ION | Authors: | Tempel, W, Yu, W, Li, Y, Blum, G, Luo, M, Pittella-Silva, F, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Brown, P.J, Structural Genomics Consortium (SGC) | Deposit date: | 2017-06-05 | Release date: | 2017-06-21 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | SETD8 in complex with a covalent inhibitor to be published
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5VAC
| Crystal Structure of ATXR5 SET domain in complex with K36me3 histone H3 peptide | Descriptor: | DIMETHYL SULFOXIDE, Histone H3.2, Probable Histone-lysine N-methyltransferase ATXR5, ... | Authors: | Bergamin, E, Sarvan, S, Malette, J, Eram, M, Yeung, S, Mongeon, V, Joshi, M, Brunzelle, J.S, Michaels, S.D, Blais, A, Vedadi, M, Couture, J.F. | Deposit date: | 2017-03-24 | Release date: | 2017-04-19 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.949 Å) | Cite: | Molecular basis for the methylation specificity of ATXR5 for histone H3. Nucleic Acids Res., 45, 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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4MI5
| 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 | Last modified: | 2024-02-28 | 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
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6YUH
| Crystal structure of SMYD3 with diperodon R enantiomer bound to allosteric site | Descriptor: | Diperodon, GLYCEROL, Histone-lysine N-methyltransferase SMYD3, ... | Authors: | Cederfelt, D, Talibov, V.O, Dobritzsch, D, Danielson, U.H. | Deposit date: | 2020-04-27 | Release date: | 2021-01-13 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (1.93 Å) | Cite: | Discovery of an Allosteric Ligand Binding Site in SMYD3 Lysine Methyltransferase. Chembiochem, 22, 2021
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5EG2
| SET7/9 N265A in complex with AdoHcy and TAF10 peptide | Descriptor: | Histone-lysine N-methyltransferase SETD7, S-ADENOSYL-L-HOMOCYSTEINE, SODIUM ION, ... | Authors: | Kroner, G.M, Fick, R.J, Trievel, R.C. | Deposit date: | 2015-10-26 | Release date: | 2016-01-13 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.55 Å) | Cite: | Sulfur-Oxygen Chalcogen Bonding Mediates AdoMet Recognition in the Lysine Methyltransferase SET7/9. Acs Chem.Biol., 11, 2016
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