6P7Z
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6PAF
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3F9X
| Structural Insights into Lysine Multiple Methylation by SET Domain Methyltransferases, SET8-Y334F / H4-Lys20me2 / AdoHcy | Descriptor: | Histone H4, Histone-lysine N-methyltransferase SETD8, S-ADENOSYL-L-HOMOCYSTEINE | Authors: | Couture, J.-F, Dirk, L.M.A, Brunzelle, J.S, Houtz, R.L, Trievel, R.C. | Deposit date: | 2008-11-14 | Release date: | 2008-11-25 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.25 Å) | Cite: | Structural origins for the product specificity of SET domain protein methyltransferases. Proc.Natl.Acad.Sci.Usa, 105, 2008
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5TEG
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2F69
| Ternary complex of SET7/9 bound to AdoHcy and a TAF10 peptide | Descriptor: | Histone-lysine N-methyltransferase, H3 lysine-4 specific SET7, S-ADENOSYL-L-HOMOCYSTEINE, ... | Authors: | Couture, J.-F, Collazo, E, Hauk, G, Trievel, R.C. | Deposit date: | 2005-11-28 | Release date: | 2006-01-17 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (1.3 Å) | Cite: | Structural basis for the methylation site specificity of SET7/9 Nat.Struct.Mol.Biol., 13, 2006
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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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3M58
| SET7/9 Y245A in complex with TAF10-K189me1 peptide and AdoHcy | Descriptor: | Histone-lysine N-methyltransferase SETD7, S-ADENOSYL-L-HOMOCYSTEINE, SULFATE ION, ... | Authors: | Del Rizzo, P.A, Couture, J.-F, Roiko, M.S, Strunk, B.S, Brunzelle, J.S, Dirk, L.M, Houtz, R.L, Trievel, R.C. | Deposit date: | 2010-03-12 | Release date: | 2010-07-28 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.4 Å) | Cite: | SET7/9 catalytic mutants reveal the role of active site water molecules in lysine multiple methylation. J.Biol.Chem., 285, 2010
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3CBP
| Set7/9-ER-Sinefungin complex | Descriptor: | BETA-MERCAPTOETHANOL, Estrogen receptor, GLYCEROL, ... | Authors: | Cheng, X, Jia, D. | Deposit date: | 2008-02-22 | Release date: | 2008-05-13 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (1.42 Å) | Cite: | Regulation of estrogen receptor alpha by the SET7 lysine methyltransferase. Mol.Cell, 30, 2008
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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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7XUD
| Structure of G9a in complex with compound 26a | Descriptor: | 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, CHLORIDE ION, ... | Authors: | Niwa, H, Shirai, F, Sato, S, Nishigaya, Y, Umehara, T. | Deposit date: | 2022-05-18 | Release date: | 2023-03-29 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (1.45 Å) | Cite: | Discovery of Novel Substrate-Competitive Lysine Methyltransferase G9a Inhibitors as Anticancer Agents. J.Med.Chem., 66, 2023
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1ZKK
| Crystal structure of hSET8 in ternary complex with H4 peptide (16-24) and AdoHcy | Descriptor: | Histone-lysine N-methyltransferase, H4 lysine-20 specific, Peptide corresponding to residues 15-24 of histone H4, ... | Authors: | Couture, J.-F, Collazo, E, Brunzelle, J.S, Trievel, R.C. | Deposit date: | 2005-05-03 | Release date: | 2005-06-07 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (1.45 Å) | Cite: | Structural and functional analysis of SET8, a histone H4 Lys-20 methyltransferase Genes Dev., 19, 2005
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5JIY
| Structure of G9a SET-domain with Histone H3K9norLeucine mutant peptide and bound S-adenosylmethionine | Descriptor: | Histone H3.1 mutant peptide with H3K9nor-leucine, Histone-lysine N-methyltransferase EHMT2, S-ADENOSYLMETHIONINE, ... | Authors: | Jayaram, H, Bellon, S.F, Poy, F. | Deposit date: | 2016-04-22 | Release date: | 2016-09-14 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (1.48 Å) | Cite: | S-adenosyl methionine is necessary for inhibition of the methyltransferase G9a by the lysine 9 to methionine mutation on histone H3. Proc.Natl.Acad.Sci.USA, 113, 2016
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7X73
| Structure of G9a in complex with RK-701 | Descriptor: | 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Histone-lysine N-methyltransferase EHMT2, ... | Authors: | Niwa, H, Shirai, F, Sato, S, Nishigaya, Y, Shirouzu, M, Umehara, T. | Deposit date: | 2022-03-09 | Release date: | 2022-12-21 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (1.49 Å) | Cite: | A specific G9a inhibitor unveils BGLT3 lncRNA as a universal mediator of chemically induced fetal globin gene expression. Nat Commun, 14, 2023
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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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2BQZ
| Crystal structure of a ternary complex of the human histone methyltransferase Pr-SET7 (also known as SET8) | Descriptor: | HISTONE H4, S-ADENOSYL-L-HOMOCYSTEINE, SET8 PROTEIN | Authors: | Xiao, B, Jing, C, Kelly, G, Walker, P.A, Muskett, F.W, Frenkiel, T.A, Martin, S.R, Sarma, K, Reinberg, D, Gamblin, S.J, Wilson, J.R. | Deposit date: | 2005-04-28 | Release date: | 2005-06-08 | Last modified: | 2011-07-13 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Specificity and Mechanism of the Histone Methyltransferase Pr-Set7 Genes Dev., 19, 2005
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5JLB
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3F9Y
| Structural Insights into Lysine Multiple Methylation by SET Domain Methyltransferases, SET8-Y334F / H4-Lys20me1 / AdoHcy | Descriptor: | Histone H4, Histone-lysine N-methyltransferase SETD8, S-ADENOSYL-L-HOMOCYSTEINE | Authors: | Couture, J.-F, Dirk, L.M.A, Brunzelle, J.S, Houtz, R.L, Trievel, R.C. | Deposit date: | 2008-11-14 | Release date: | 2008-11-25 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Structural origins for the product specificity of SET domain protein methyltransferases. Proc.Natl.Acad.Sci.Usa, 105, 2008
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5CCL
| Crystal structure of SMYD3 with SAM and oxindole compound | Descriptor: | 1,2-ETHANEDIOL, 2-oxidanylidene-N-piperidin-4-yl-1,3-dihydroindole-5-carboxamide, Histone-lysine N-methyltransferase SMYD3, ... | Authors: | Boriack-Sjodin, P.A. | Deposit date: | 2015-07-02 | Release date: | 2015-09-09 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor. Acs Med.Chem.Lett., 7, 2016
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5LT7
| Structure of the Epigenetic Oncogene MMSET and inhibition by N-Alkyl Sinefungin Derivatives | Descriptor: | Histone-lysine N-methyltransferase SETD2, THIOCYANATE ION, ZINC ION, ... | Authors: | Tisi, D, Pathuri, P, Heightman, T. | Deposit date: | 2016-09-06 | Release date: | 2016-10-05 | Last modified: | 2019-10-16 | Method: | X-RAY DIFFRACTION (1.51 Å) | Cite: | Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives. ACS Chem. Biol., 11, 2016
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7O2C
| X-RAY STRUCTURE OF SMYD3 IN COMPLEX WITH the benzodiazepine-based probe BAY-6035 | Descriptor: | (2S)-1-[[(1R,5S)-3-azabicyclo[3.1.0]hexan-3-yl]carbonyl]-N-(2-cyclopropylethyl)-2-methyl-4-oxidanylidene-3,5-dihydro-2H-1,5-benzodiazepine-7-carboxamide, Histone-lysine N-methyltransferase SMYD3, S-ADENOSYLMETHIONINE, ... | Authors: | Steuber, H. | Deposit date: | 2021-03-30 | Release date: | 2021-07-07 | Last modified: | 2021-09-22 | Method: | X-RAY DIFFRACTION (1.52 Å) | Cite: | Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening. Slas Discov, 26, 2021
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3QWP
| Crystal structure of SET and MYND domain containing 3; Zinc finger MYND domain-containing protein 1 | Descriptor: | GLYCEROL, S-ADENOSYLMETHIONINE, SET and MYND domain-containing protein 3, ... | Authors: | Dong, A, Dombrovski, L, Li, Y, Wernimont, A, Weigelt, J, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Min, J, Wu, H, Structural Genomics Consortium (SGC) | Deposit date: | 2011-02-28 | Release date: | 2011-04-06 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (1.53 Å) | Cite: | The Crystal Structure of human Histone-lysine N-methyltransferase SMYD3 To be Published
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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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6P6K
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6ZRB
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3M55
| SET7/9 Y305F in complex with TAF10-K189me1 peptide and AdoHcy | Descriptor: | Histone-lysine N-methyltransferase SETD7, S-ADENOSYL-L-HOMOCYSTEINE, TAF10 peptide | Authors: | Del Rizzo, P.A, Couture, J.-F, Roiko, M.S, Strunk, B.S, Brunzelle, J.S, Dirk, L.M, Houtz, R.L, Trievel, R.C. | Deposit date: | 2010-03-12 | Release date: | 2010-07-28 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.55 Å) | Cite: | SET7/9 catalytic mutants reveal the role of active site water molecules in lysine multiple methylation. J.Biol.Chem., 285, 2010
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