4X61
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![BU of 4x61 by Molmil](/molmil-images/mine/4x61) | Crystal structure of PRMT5:MEP50 with EPZ015666 and SAM | 分子名称: | GLYCEROL, Methylosome protein 50, N-[(2S)-3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl]-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide, ... | 著者 | Boriack-Sjodin, P.A. | 登録日 | 2014-12-06 | 公開日 | 2015-04-22 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | 主引用文献 | A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat.Chem.Biol., 11, 2015
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6CKC
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![BU of 6ckc by Molmil](/molmil-images/mine/6ckc) | Structure of PRMT5:MEP50 in complex with LLY-283, a potent and selective inhibitor of PRMT5, with antitumor activity | 分子名称: | 7-[(5R)-5-C-phenyl-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine, Methylosome protein 50, Protein arginine N-methyltransferase 5 | 著者 | Antonysamy, S. | 登録日 | 2018-02-27 | 公開日 | 2018-05-16 | 最終更新日 | 2024-03-13 | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | 主引用文献 | LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. ACS Med Chem Lett, 9, 2018
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6K1S
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![BU of 6k1s by Molmil](/molmil-images/mine/6k1s) | Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase (PRMT5) Inhibitors | 分子名称: | 1,2-ETHANEDIOL, 2-[[7-[(2~{R},3~{R},4~{S},5~{R})-5-[(~{R})-(4-chlorophenyl)-oxidanyl-methyl]-3,4-bis(oxidanyl)oxolan-2-yl]pyrrolo[2,3-d]pyrimidin-4-yl]amino]ethanal, DIMETHYL SULFOXIDE, ... | 著者 | Tong, S, Lin, H. | 登録日 | 2019-05-12 | 公開日 | 2019-06-19 | 最終更新日 | 2023-11-22 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors. Acs Med.Chem.Lett., 10, 2019
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7BOC
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![BU of 7boc by Molmil](/molmil-images/mine/7boc) | Crystal structure of the PRMT5 TIM barrel domain in complex with RioK1 peptide | 分子名称: | Protein arginine N-methyltransferase 5, peptide | 著者 | Krzyzanowski, A, t Hart, P, Waldmann, H, Gasper, R. | 登録日 | 2021-01-25 | 公開日 | 2021-09-15 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | 主引用文献 | Biochemical Investigation of the Interaction of pICln, RioK1 and COPR5 with the PRMT5-MEP50 Complex. Chembiochem, 22, 2021
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5FA5
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![BU of 5fa5 by Molmil](/molmil-images/mine/5fa5) | |
8CSG
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![BU of 8csg by Molmil](/molmil-images/mine/8csg) | Human PRMT5:MEP50 structure with Fragment 1 and MTA Bound | 分子名称: | 1,2-ETHANEDIOL, 5'-DEOXY-5'-METHYLTHIOADENOSINE, 6-bromo-1H-pyrrolo[3,2-b]pyridin-5-amine, ... | 著者 | Gunn, R.J, Lawson, J.D, Smith, C.R. | 登録日 | 2022-05-12 | 公開日 | 2022-10-05 | 最終更新日 | 2024-05-22 | 実験手法 | X-RAY DIFFRACTION (2.48 Å) | 主引用文献 | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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8CTB
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![BU of 8ctb by Molmil](/molmil-images/mine/8ctb) | Human PRMT5:MEP50 structure with Fragment 3 and MTA Bound | 分子名称: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, 7-chloro-1-methyl-1H-benzimidazol-2-amine, Methylosome protein 50, ... | 著者 | Gunn, R.J, Lawson, J.D, Smith, C.R. | 登録日 | 2022-05-13 | 公開日 | 2022-10-05 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (2.61 Å) | 主引用文献 | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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4G56
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![BU of 4g56 by Molmil](/molmil-images/mine/4g56) | Crystal Structure of full length PRMT5/MEP50 complexes from Xenopus laevis | 分子名称: | Hsl7 protein, MGC81050 protein, S-ADENOSYL-L-HOMOCYSTEINE | 著者 | Ho, M, Wilczek, C, Bonanno, J, Shechter, D, Almo, S.C, New York Structural Genomics Research Consortium (NYSGRC) | 登録日 | 2012-07-17 | 公開日 | 2012-10-03 | 最終更新日 | 2017-11-15 | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | 主引用文献 | Structure of the arginine methyltransferase PRMT5-MEP50 reveals a mechanism for substrate specificity Plos One, 8, 2013
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7UYF
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![BU of 7uyf by Molmil](/molmil-images/mine/7uyf) | Human PRMT5:MEP50 structure with Fragment 4 and MTA Bound | 分子名称: | 4-methyl-1,5-naphthyridin-2-amine, 5'-DEOXY-5'-METHYLTHIOADENOSINE, CHLORIDE ION, ... | 著者 | Gunn, R.J, Lawson, J.D, Smith, C.R. | 登録日 | 2022-05-06 | 公開日 | 2022-10-05 | 最終更新日 | 2024-05-22 | 実験手法 | X-RAY DIFFRACTION (2.82 Å) | 主引用文献 | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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7UY1
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![BU of 7uy1 by Molmil](/molmil-images/mine/7uy1) | HUMAN PRMT5:MEP50 COMPLEX WITH MTA and Fragment 5 Bound | 分子名称: | 1,2-ETHANEDIOL, 3-methyl-1,5-naphthyridin-2-amine, 5'-DEOXY-5'-METHYLTHIOADENOSINE, ... | 著者 | Gunn, R.J. | 登録日 | 2022-05-06 | 公開日 | 2022-10-05 | 最終更新日 | 2024-05-22 | 実験手法 | X-RAY DIFFRACTION (2.66 Å) | 主引用文献 | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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5EMM
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![BU of 5emm by Molmil](/molmil-images/mine/5emm) | |
5EML
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![BU of 5eml by Molmil](/molmil-images/mine/5eml) | |
5EMK
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![BU of 5emk by Molmil](/molmil-images/mine/5emk) | |
5EMJ
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![BU of 5emj by Molmil](/molmil-images/mine/5emj) | |
4GQB
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![BU of 4gqb by Molmil](/molmil-images/mine/4gqb) | Crystal Structure of the human PRMT5:MEP50 Complex | 分子名称: | (2S,5S,6E)-2,5-diamino-6-[(3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxydihydrofuran-2(3H)-ylidene]hexanoic acid, Histone H4 peptide, Methylosome protein 50, ... | 著者 | Antonysamy, S, Bonday, Z, Campbell, R, Doyle, B, Druzina, Z, Gheyi, T, Han, B, Jungheim, L.N, Qian, Y, Rauch, C, Russell, M, Sauder, J.M, Wasserman, S.R, Weichert, K, Willard, F.S, Zhang, A, Emtage, S. | 登録日 | 2012-08-22 | 公開日 | 2012-10-17 | 最終更新日 | 2018-11-21 | 実験手法 | X-RAY DIFFRACTION (2.06 Å) | 主引用文献 | Crystal structure of the human PRMT5:MEP50 complex. Proc.Natl.Acad.Sci.USA, 109, 2012
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8VEW
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![BU of 8vew by Molmil](/molmil-images/mine/8vew) | Crystal structure of PRMT5:MEP50 in complex with MTA and oxamide compound 24 | 分子名称: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, 5-{2-[(2R,5S)-5-methyl-2-phenylpiperidin-1-yl](oxo)acetamido}pyridine-3-carboxamide, CHLORIDE ION, ... | 著者 | Whittington, D.A. | 登録日 | 2023-12-20 | 公開日 | 2024-04-24 | 最終更新日 | 2024-05-08 | 実験手法 | X-RAY DIFFRACTION (2.69 Å) | 主引用文献 | Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP -Deleted Cancers. J.Med.Chem., 67, 2024
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8VEU
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![BU of 8veu by Molmil](/molmil-images/mine/8veu) | |
8VEO
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![BU of 8veo by Molmil](/molmil-images/mine/8veo) | Crystal structure of PRMT5:MEP50 in complex with MTA | 分子名称: | 1,2-ETHANEDIOL, 5'-DEOXY-5'-METHYLTHIOADENOSINE, DI(HYDROXYETHYL)ETHER, ... | 著者 | Whittington, D.A. | 登録日 | 2023-12-20 | 公開日 | 2024-04-24 | 最終更新日 | 2024-05-08 | 実験手法 | X-RAY DIFFRACTION (2.03 Å) | 主引用文献 | Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP -Deleted Cancers. J.Med.Chem., 67, 2024
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8VEY
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![BU of 8vey by Molmil](/molmil-images/mine/8vey) | |
8VET
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![BU of 8vet by Molmil](/molmil-images/mine/8vet) | |
8VEX
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![BU of 8vex by Molmil](/molmil-images/mine/8vex) | |
7ZUP
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![BU of 7zup by Molmil](/molmil-images/mine/7zup) | Human PRMT5:MEP50 structure with Fragment (Example 18) and MTA Bound | 分子名称: | 3-ethylimidazo[4,5-b]pyridin-2-amine, 5'-DEOXY-5'-METHYLTHIOADENOSINE, GLYCEROL, ... | 著者 | Ahmad, M.U, Koelmel, W, Arkhipova, V, Lawson, J.D, Smith, C.R, Gunn, R.J. | 登録日 | 2022-05-12 | 公開日 | 2022-10-19 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | 主引用文献 | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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7ZVU
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![BU of 7zvu by Molmil](/molmil-images/mine/7zvu) | HUMAN PRMT5:MEP50 Crystal Structure With MTA and Fragment Bound | 分子名称: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, GLYCEROL, Methylosome protein 50, ... | 著者 | Ahmad, M.U, Koelmel, W, Arkhipova, V, Lawson, J.D, Smith, C.R, Gunn, R.J. | 登録日 | 2022-05-17 | 公開日 | 2022-10-19 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | 主引用文献 | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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7ZUU
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![BU of 7zuu by Molmil](/molmil-images/mine/7zuu) | HUMAN PRMT5:MEP50 Crystal Structure With MTA and Fragment Bound | 分子名称: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, GLYCEROL, Methylosome protein 50, ... | 著者 | Ahmad, M.U, Koelmel, W, Arkhipova, V, Lawson, J.D, Smith, C.R, Gunn, R.J. | 登録日 | 2022-05-13 | 公開日 | 2022-10-19 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2.09 Å) | 主引用文献 | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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7ZV2
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![BU of 7zv2 by Molmil](/molmil-images/mine/7zv2) | HUMAN PRMT5:MEP50 Crystal Structure With MTA and Fragment Bound | 分子名称: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, GLYCEROL, Methylosome protein 50, ... | 著者 | Ahmad, M.U, Koelmel, W, Arkhipova, V, Lawson, J.D, Smith, C.R, Gunn, R.J. | 登録日 | 2022-05-13 | 公開日 | 2022-10-19 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | 主引用文献 | Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. Rsc Med Chem, 13, 2022
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