6MBP
 
 | | GLP Methyltransferase with Inhibitor EML741- P3121 Crystal Form | | 分子名称: | 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, ... | | 著者 | Horton, J.R, Cheng, X. | | 登録日 | 2018-08-30 | | 公開日 | 2019-02-27 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (1.947 Å) | | 主引用文献 | 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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6AGO
 | | Crystal structure of MRG15-ASH1L Histone methyltransferase complex | | 分子名称: | Histone-lysine N-methyltransferase ASH1L, Mortality factor 4 like 1, S-ADENOSYLMETHIONINE, ... | | 著者 | Lee, Y, Song, J. | | 登録日 | 2018-08-13 | | 公開日 | 2019-03-13 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (3.103 Å) | | 主引用文献 | Structural Basis of MRG15-Mediated Activation of the ASH1L Histone Methyltransferase by Releasing an Autoinhibitory Loop.
Structure, 27, 2019
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6A5M
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6A5N
 | | Crystal structure of Arabidopsis thaliana SUVH6 in complex with methylated DNA | | 分子名称: | DNA (5'-D(*CP*AP*CP*TP*GP*CP*TP*GP*AP*GP*TP*AP*CP*T)-3'), DNA (5'-D(*GP*AP*GP*TP*AP*CP*TP*(5CM)P*AP*GP*CP*AP*GP*T)-3'), Histone-lysine N-methyltransferase, ... | | 著者 | Li, X, Du, J. | | 登録日 | 2018-06-24 | | 公開日 | 2018-08-29 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Mechanistic insights into plant SUVH family H3K9 methyltransferases and their binding to context-biased non-CG DNA methylation.
Proc. Natl. Acad. Sci. U.S.A., 115, 2018
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6A5K
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6CHG
 | | Crystal structure of the yeast COMPASS catalytic module | | 分子名称: | H3, Histone-lysine N-methyltransferase, H3 lysine-4 specific, ... | | 著者 | Hsu, P.L, Li, H, Zheng, N. | | 登録日 | 2018-02-22 | | 公開日 | 2018-08-22 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.985 Å) | | 主引用文献 | Crystal Structure of the COMPASS H3K4 Methyltransferase Catalytic Module.
Cell, 174, 2018
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6CEN
 | | Crystal Structure of WHSC1L1 in Complex with Inhibitor PEP21 | | 分子名称: | ACE-GLY-VAL-NLE-ARG-ILE-NH2, Histone-lysine N-methyltransferase NSD3, S-ADENOSYLMETHIONINE, ... | | 著者 | Boriack-Sjodin, P.A, Swinger, K, Farrow, N.A. | | 登録日 | 2018-02-12 | | 公開日 | 2018-05-09 | | 最終更新日 | 2018-05-23 | | 実験手法 | X-RAY DIFFRACTION (1.61 Å) | | 主引用文献 | Identification of a peptide inhibitor for the histone methyltransferase WHSC1.
PLoS ONE, 13, 2018
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6CBX
 | | Crystal structure of human SET and MYND Domain Containing protein 2 with MTF1497 | | 分子名称: | 1,2-ETHANEDIOL, CHLORIDE ION, N-lysine methyltransferase SMYD2, ... | | 著者 | ZENG, H, DONG, A, Hutchinson, 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) | | 登録日 | 2018-02-05 | | 公開日 | 2018-03-14 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (1.94 Å) | | 主引用文献 | Crystal structure of human SET and MYND Domain Containing protein 2 with MTF1497
to be published
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6CBY
 | | Crystal structure of human SET and MYND Domain Containing protein 2 with MTF9975 | | 分子名称: | N-lysine methyltransferase SMYD2, ZINC ION, [3-(4-amino-6-methyl-1H-imidazo[4,5-c]pyridin-1-yl)-3-methylazetidin-1-yl][1-({1-[(1R)-cyclohept-2-en-1-yl]piperidin-4-yl}methyl)-1H-pyrrol-3-yl]methanone | | 著者 | ZENG, H, DONG, A, Hutchinson, 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) | | 登録日 | 2018-02-05 | | 公開日 | 2018-03-14 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | | 主引用文献 | Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.
J.Med.Chem., 62, 2019
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6FND
 | | Crystal structure of Toxoplasma gondii AKMT | | 分子名称: | 1,2-ETHANEDIOL, Apical complex lysine methyltransferase, DI(HYDROXYETHYL)ETHER, ... | | 著者 | Pivovarova, Y, Dong, G. | | 登録日 | 2018-02-02 | | 公開日 | 2018-11-14 | | 実験手法 | X-RAY DIFFRACTION (2.101 Å) | | 主引用文献 | Structure of a Novel Dimeric SET Domain Methyltransferase that Regulates Cell Motility.
J. Mol. Biol., 430, 2018
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6C24
 | | Cryo-EM structure of PRC2 bound to cofactors AEBP2 and JARID2 in the Extended Active State | | 分子名称: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH2, JARID2-substrate, ... | | 著者 | Kasinath, V, Faini, M, Poepsel, S, Reif, D, Feng, A, Stjepanovic, G, Aebersold, R, Nogales, E. | | 登録日 | 2018-01-06 | | 公開日 | 2018-01-24 | | 最終更新日 | 2019-12-18 | | 実験手法 | ELECTRON MICROSCOPY (3.5 Å) | | 主引用文献 | Structures of human PRC2 with its cofactors AEBP2 and JARID2.
Science, 359, 2018
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6C23
 | | Cryo-EM structure of PRC2 bound to cofactors AEBP2 and JARID2 in the Compact Active State | | 分子名称: | Histone-binding protein RBBP4, Histone-lysine N-methyltransferase EZH2, JARID2-substrate, ... | | 著者 | Kasinath, V, Faini, M, Poepsel, S, Reif, D, Feng, A, Stjepanovic, G, Aebersold, R, Nogales, E. | | 登録日 | 2018-01-05 | | 公開日 | 2018-01-24 | | 最終更新日 | 2019-12-18 | | 実験手法 | ELECTRON MICROSCOPY (3.9 Å) | | 主引用文献 | Structures of human PRC2 with its cofactors AEBP2 and JARID2.
Science, 359, 2018
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6BX3
 | | Structure of histone H3k4 methyltransferase | | 分子名称: | COMPASS component BRE2, COMPASS component SDC1, COMPASS component SPP1, ... | | 著者 | Skiniotis, G, Qu, Q.H. | | 登録日 | 2017-12-16 | | 公開日 | 2018-09-05 | | 最終更新日 | 2024-03-13 | | 実験手法 | ELECTRON MICROSCOPY (4.3 Å) | | 主引用文献 | Structure and Conformational Dynamics of a COMPASS Histone H3K4 Methyltransferase Complex.
Cell, 174, 2018
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6BOX
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6BOZ
 | | Structure of human SETD8 in complex with covalent inhibitor MS4138 | | 分子名称: | 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 | | 著者 | Babault, N, Anqi, M, Jin, J. | | 登録日 | 2017-11-21 | | 公開日 | 2019-05-01 | | 最終更新日 | 2019-12-04 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | The dynamic conformational landscape of the protein methyltransferase SETD8.
Elife, 8, 2019
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6BP4
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5YLT
 | | Crystal structure of SET7/9 in complex with a cyproheptadine derivative | | 分子名称: | 2-(1-methylpiperidin-4-ylidene)tricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-6-ol, GLYCEROL, Histone-lysine N-methyltransferase SETD7, ... | | 著者 | Hirano, T, Fujiwara, T, Niwa, H, Hirano, M, Ohira, K, Okazaki, Y, Sato, S, Umehara, T, Maemoto, Y, Ito, A, Yoshida, M, Kagechika, H. | | 登録日 | 2017-10-19 | | 公開日 | 2018-06-20 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.69 Å) | | 主引用文献 | Development of Novel Inhibitors for Histone Methyltransferase SET7/9 based on Cyproheptadine.
ChemMedChem, 13, 2018
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5YJO
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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 | | 分子名称: | 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, ... | | 著者 | Gajiwala, K.S, Brooun, A, Liu, W, Deng, Y, Stewart, A.E. | | 登録日 | 2017-09-25 | | 公開日 | 2017-12-27 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.81 Å) | | 主引用文献 | 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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6B3W
 | | Structure of Hs/AcPRC2 in complex with 5,8-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one | | 分子名称: | 5,8-dichloro-7-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one, Enhancer of zeste 2 polycomb repressive complex 2 subunit,Enhancer of zeste 2 polycomb repressive complex 2 subunit, Polycomb protein EED, ... | | 著者 | Gajiwala, K.S, Brooun, A, Liu, W, Deng, Y, Stewart, A.E. | | 登録日 | 2017-09-25 | | 公開日 | 2017-12-27 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.05 Å) | | 主引用文献 | 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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5WG6
 | | Human Polycomb Repressive Complex 2 in complex with GSK126 inhibitor | | 分子名称: | 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3-methyl-6-[6-(piperazin-1-yl)pyridin-3-yl]-1H-indole-4-carboxamide, Histone-lysine N-methyltransferase EZH2,Polycomb protein SUZ12 (E.C.2.1.1.43) chimera, Polycomb protein EED, ... | | 著者 | Bratkowski, M.A, Liu, X. | | 登録日 | 2017-07-13 | | 公開日 | 2018-06-27 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.901 Å) | | 主引用文献 | An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
Sci Rep, 8, 2018
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5WFC
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5WFD
 | | Humanized mutant of the Chaetomium thermophilum Polycomb Repressive Complex 2 bound to the inhibitor GSK126 | | 分子名称: | 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3-methyl-6-[6-(piperazin-1-yl)pyridin-3-yl]-1H-indole-4-carboxamide, Histone-lysine-N-methyltransferase EZH2, Polycomb protein SUZ12 chimera, ... | | 著者 | Bratkowski, M.A, Liu, X. | | 登録日 | 2017-07-11 | | 公開日 | 2018-06-27 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.654 Å) | | 主引用文献 | An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
Sci Rep, 8, 2018
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5WF7
 | | Chaetomium thermophilum Polycomb Repressive Complex 2 bound to GSK126 | | 分子名称: | 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3-methyl-6-[6-(piperazin-1-yl)pyridin-3-yl]-1H-indole-4-carboxamide, Histone-lysine-N-methyltransferase EZH2, Polycomb protein SUZ12 chimera, ... | | 著者 | Bratkowski, M.A, Liu, X. | | 登録日 | 2017-07-11 | | 公開日 | 2018-06-27 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | An Evolutionarily Conserved Structural Platform for PRC2 Inhibition by a Class of Ezh2 Inhibitors.
Sci Rep, 8, 2018
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5XXJ
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