5KJM
 
 | | SMYD2 in complex with AZ931 | | 分子名称: | 6-[2-[4-[2-(3,4-dichlorophenyl)ethyl]piperazin-1-yl]phenyl]-~{N}-(3-pyrrolidin-1-ylpropyl)-2~{H}-pyrazolo[3,4-b]pyridine-4-carboxamide, N-lysine methyltransferase SMYD2, S-ADENOSYLMETHIONINE, ... | | 著者 | Ferguson, A. | | 登録日 | 2016-06-20 | | 公開日 | 2016-12-07 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.19 Å) | | 主引用文献 | Design, Synthesis, and Biological Activity of Substrate Competitive SMYD2 Inhibitors.
J. Med. Chem., 59, 2016
|
|
5KJI
 | |
5JLE
 | | Crystal structure of SETD2 bound to SAH | | 分子名称: | Histone-lysine N-methyltransferase SETD2, S-ADENOSYL-L-HOMOCYSTEINE, ZINC ION | | 著者 | Li, H, Yang, S, Zheng, X. | | 登録日 | 2016-04-27 | | 公開日 | 2016-11-02 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Molecular basis for oncohistone H3 recognition by SETD2 methyltransferase
Genes Dev., 30, 2016
|
|
5JLB
 | |
5JJY
 | | Crystal structure of SETD2 bound to histone H3.3 K36M peptide | | 分子名称: | Histone H3.3, Histone-lysine N-methyltransferase SETD2, S-ADENOSYL-L-HOMOCYSTEINE, ... | | 著者 | Yang, S, Zheng, X, Li, H. | | 登録日 | 2016-04-25 | | 公開日 | 2016-11-02 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.053 Å) | | 主引用文献 | Molecular basis for oncohistone H3 recognition by SETD2 methyltransferase
Genes Dev., 30, 2016
|
|
5JIY
 | | Structure of G9a SET-domain with Histone H3K9norLeucine mutant peptide and bound S-adenosylmethionine | | 分子名称: | Histone H3.1 mutant peptide with H3K9nor-leucine, Histone-lysine N-methyltransferase EHMT2, S-ADENOSYLMETHIONINE, ... | | 著者 | Jayaram, H, Bellon, S.F, Poy, F. | | 登録日 | 2016-04-22 | | 公開日 | 2016-09-14 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (1.48 Å) | | 主引用文献 | 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
|
|
5JIN
 | | Structure of G9a SET-domain with Histone H3K9M mutant peptide and bound S-adenosylmethionine | | 分子名称: | Histone H3.1 peptide with K9M mutation, Histone-lysine N-methyltransferase EHMT2, S-ADENOSYLMETHIONINE, ... | | 著者 | Jayaram, H, Bellon, S.F, Poy, F. | | 登録日 | 2016-04-22 | | 公開日 | 2016-07-06 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | 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
|
|
5JJ0
 | | Structure of G9a SET-domain with Histone H3K9M peptide and excess SAH | | 分子名称: | Histone H3K9M mutant peptide, Histone-lysine N-methyltransferase EHMT2, S-ADENOSYLMETHIONINE, ... | | 著者 | Jayaram, H, Bellon, S.F, Poy, F. | | 登録日 | 2016-04-22 | | 公開日 | 2016-07-06 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.72 Å) | | 主引用文献 | 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
|
|
5JHN
 | | Structure of G9a SET-domain with Histone H3K9Ala mutant peptide and bound S-adenosylmethionine | | 分子名称: | Histone H3.1 peptide with K9A mutation, Histone-lysine N-methyltransferase EHMT2, S-ADENOSYLMETHIONINE, ... | | 著者 | Jayaram, H, Bellon, S.F, Poy, F. | | 登録日 | 2016-04-21 | | 公開日 | 2016-07-06 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.67 Å) | | 主引用文献 | 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
|
|
5IJ7
 | | Structure of Hs/AcPRC2 in complex with a pyridone inhibitor | | 分子名称: | 5,8-dichloro-2-[(4-ethyl-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-({1-[(2R)-2-hydroxypropanoyl]piperidin-4-yl}oxy)-3,4-dihydroisoquinolin-1(2H)-one, Enhancer of Zeste Homolog 2 (EZH2),Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, ... | | 著者 | Gajiwala, K.S, Brooun, A, Deng, Y.-L, Liu, W. | | 登録日 | 2016-03-01 | | 公開日 | 2016-05-04 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.62 Å) | | 主引用文献 | Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.
Nat Commun, 7, 2016
|
|
5IJ8
 | | Structure of the primary oncogenic mutant Y641N Hs/AcPRC2 in complex with a pyridone inhibitor | | 分子名称: | 5,8-dichloro-2-[(4-ethyl-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-({1-[(2R)-2-hydroxypropanoyl]piperidin-4-yl}oxy)-3,4-dihydroisoquinolin-1(2H)-one, Enhancer of Zeste Homolog 2 (EZH2),Histone-lysine N-methyltransferase EZH2, Polycomb protein EED, ... | | 著者 | Gajiwala, K.S, Brooun, A, Deng, Y.-L, Liu, W. | | 登録日 | 2016-03-01 | | 公開日 | 2016-05-04 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.99 Å) | | 主引用文献 | Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.
Nat Commun, 7, 2016
|
|
5HYN
 | | Structure of Human Polycomb Repressive Complex 2 (PRC2) with oncogenic histone H3K27M peptide | | 分子名称: | H3K27M, Histone-lysine N-methyltransferase EZH2, JARID2 K116me3, ... | | 著者 | Zhang, Y, Justin, N, Wilson, J.R, Gamblin, S.J. | | 登録日 | 2016-02-01 | | 公開日 | 2016-05-11 | | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | | 主引用文献 | Structural basis of oncogenic histone H3K27M inhibition of human polycomb repressive complex 2.
Nat Commun, 7, 2016
|
|
5HT6
 | | Crystal structure of the SET domain of the human MLL5 methyltransferase | | 分子名称: | Histone-lysine N-methyltransferase 2E | | 著者 | le Maire, A, Mas-y-Mas, S, Dumas, C, Lebedev, A. | | 登録日 | 2016-01-26 | | 公開日 | 2016-11-16 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.093 Å) | | 主引用文献 | 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
|
|
5HQ2
 | | Structural model of Set8 histone H4 Lys20 methyltransferase bound to nucleosome core particle | | 分子名称: | DNA (149-MER), Guanine nucleotide exchange factor SRM1, Histone H2A, ... | | 著者 | Tavarekere, G, McGinty, R.K, Tan, S. | | 登録日 | 2016-01-21 | | 公開日 | 2016-03-23 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (4.5 Å) | | 主引用文献 | Multivalent Interactions by the Set8 Histone Methyltransferase With Its Nucleosome Substrate.
J.Mol.Biol., 428, 2016
|
|
5HQ8
 | |
5HI7
 | | Co-crystal structure of human SMYD3 with an aza-SAH compound | | 分子名称: | 5'-{[(3S)-3-amino-3-carboxypropyl][3-(dimethylamino)propyl]amino}-5'-deoxyadenosine, DIMETHYL SULFOXIDE, Histone-lysine N-methyltransferase SMYD3, ... | | 著者 | Elkins, P.A, Bonnette, W.G. | | 登録日 | 2016-01-11 | | 公開日 | 2016-03-30 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | | 主引用文献 | Structure-Based Design of a Novel SMYD3 Inhibitor that Bridges the SAM-and MEKK2-Binding Pockets.
Structure, 24, 2016
|
|
5F6L
 | | The crystal structure of MLL1 (N3861I/Q3867L) in complex with RbBP5 and Ash2L | | 分子名称: | Histone-lysine N-methyltransferase 2A, Retinoblastoma-binding protein 5, S-ADENOSYL-L-HOMOCYSTEINE, ... | | 著者 | Li, Y, Lei, M, Chen, Y. | | 登録日 | 2015-12-06 | | 公開日 | 2016-02-24 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Structural basis for activity regulation of MLL family methyltransferases.
Nature, 530, 2016
|
|
5F6K
 | | Crystal structure of the MLL3-Ash2L-RbBP5 complex | | 分子名称: | Histone-lysine N-methyltransferase 2C, Retinoblastoma-binding protein 5, S-ADENOSYL-L-HOMOCYSTEINE, ... | | 著者 | Li, Y, Lei, M, Chen, Y. | | 登録日 | 2015-12-06 | | 公開日 | 2016-02-24 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.411 Å) | | 主引用文献 | Structural basis for activity regulation of MLL family methyltransferases.
Nature, 530, 2016
|
|
5F59
 | | The crystal structure of MLL3 SET domain | | 分子名称: | Histone-lysine N-methyltransferase 2C, S-ADENOSYL-L-HOMOCYSTEINE, ZINC ION | | 著者 | Li, Y, Lei, M, Chen, Y. | | 登録日 | 2015-12-04 | | 公開日 | 2016-02-24 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (2.801 Å) | | 主引用文献 | Structural basis for activity regulation of MLL family methyltransferases.
Nature, 530, 2016
|
|
5F5E
 | |
5EX0
 | | Crystal structure of human SMYD3 in complex with a MAP3K2 peptide | | 分子名称: | ACETIC ACID, Histone-lysine N-methyltransferase SMYD3, MAP3K2 peptide, ... | | 著者 | Fu, W, Liu, N, Qiao, Q, Wang, M, Min, J, Zhu, B, Xu, R.M, Yang, N. | | 登録日 | 2015-11-23 | | 公開日 | 2016-03-09 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Structural Basis for Substrate Preference of SMYD3, a SET Domain-containing Protein Lysine Methyltransferase
J.Biol.Chem., 291, 2016
|
|
5EX3
 | | Crystal structure of human SMYD3 in complex with a VEGFR1 peptide | | 分子名称: | ACETIC ACID, Histone-lysine N-methyltransferase SMYD3, S-ADENOSYL-L-HOMOCYSTEINE, ... | | 著者 | Qiao, Q, Fu, W, Liu, N, Wang, M, Min, J, Zhu, B, Xu, R.M, Yang, N. | | 登録日 | 2015-11-23 | | 公開日 | 2016-03-09 | | 最終更新日 | 2017-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.408 Å) | | 主引用文献 | Structural Basis for Substrate Preference of SMYD3, a SET Domain-containing Protein Lysine Methyltransferase
J.Biol.Chem., 291, 2016
|
|
5EG2
 | | SET7/9 N265A in complex with AdoHcy and TAF10 peptide | | 分子名称: | Histone-lysine N-methyltransferase SETD7, S-ADENOSYL-L-HOMOCYSTEINE, SODIUM ION, ... | | 著者 | Kroner, G.M, Fick, R.J, Trievel, R.C. | | 登録日 | 2015-10-26 | | 公開日 | 2016-01-13 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | Sulfur-Oxygen Chalcogen Bonding Mediates AdoMet Recognition in the Lysine Methyltransferase SET7/9.
Acs Chem.Biol., 11, 2016
|
|
5ARG
 | | SMYD2 in complex with SGC probe BAY-598 | | 分子名称: | GLYCEROL, N-LYSINE METHYLTRANSFERASE SMYD2, N-[1-(N'-CYANO-N-[3-(DIFLUOROMETHOXY)PHENYL]CARBAMIMIDOYL)-3-(3,4-DICHLOROPHENYL)-4,5-DIHYDRO-1H-PYRAZOL-4-YL]-N-ETHYL-2-HYDROXYACETAMIDE, ... | | 著者 | Hillig, R.C, Badock, V, Barak, N, Stellfeld, T, Eggert, E, ter Laak, A, Weiske, J, Christ, C.D, Koehr, S, Stoeckigt, D, Mowat, J, Mueller, T, Fernandez-Montalvan, A.E, Hartung, I.V, Stresemann, C, Brumby, T, Weinmann, H. | | 登録日 | 2015-09-24 | | 公開日 | 2016-04-27 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | | 主引用文献 | Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (Bay-598) for the Protein Lysine Methyltransferase Smyd2.
J.Med.Chem., 59, 2016
|
|
5ARF
 | | SMYD2 in complex with small molecule inhibitor compound-2 | | 分子名称: | N-LYSINE METHYLTRANSFERASE SMYD2, N-[3-(4-CHLOROPHENYL)-1-{N'-CYANO-N-[3-(DIFLUOROMETHOXY)PHENYL]CARBAMIMIDOYL}-4,5-DIHYDRO-1H- PYRAZOL-4-YL]-N-ETHYL-2-HYDROXYACETAMIDE, S-ADENOSYLMETHIONINE, ... | | 著者 | Hillig, R.C, Badock, V, Barak, N, Stellfeld, T, Eggert, E, ter Laak, A, Weiske, J, Christ, C.D, Koehr, S, Stoeckigt, D, Mowat, J, Mueller, T, Fernandez-Montalvan, A.E, Hartung, I.V, Stresemann, C, Brumby, T, Weinmann, H. | | 登録日 | 2015-09-24 | | 公開日 | 2016-04-27 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.92 Å) | | 主引用文献 | Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (Bay-598) for the Protein Lysine Methyltransferase Smyd2.
J.Med.Chem., 59, 2016
|
|
