6V0P
 
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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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7ZUY
 | | 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 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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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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7S0U
 | | PRMT5/MEP50 crystal structure with MTA and phthalazinone fragment bound | | 分子名称: | 1,2-ETHANEDIOL, 4-(aminomethyl)phthalazin-1(2H)-one, 5'-DEOXY-5'-METHYLTHIOADENOSINE, ... | | 著者 | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Smith, C.R, Kulyk, S, Marx, M.A. | | 登録日 | 2021-08-31 | | 公開日 | 2022-01-26 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | | 主引用文献 | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers.
J.Med.Chem., 65, 2022
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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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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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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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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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7S1R
 | | PRMT5/MEP50 crystal structure with MTA and a phthalazinone inhibitor bound (compound (M)-31) | | 分子名称: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, Methylosome protein 50, Protein arginine N-methyltransferase 5, ... | | 著者 | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Kulyk, S, Smith, C.R, Marx, M.A. | | 登録日 | 2021-09-02 | | 公開日 | 2022-01-26 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers.
J.Med.Chem., 65, 2022
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6V0N
 | | PRMT5 bound to PBM peptide from Riok1 | | 分子名称: | Methylosome protein 50, Protein arginine N-methyltransferase 5, Riok1 PBM peptide, ... | | 著者 | McMIllan, B.J, Raymond, D.D. | | 登録日 | 2019-11-19 | | 公開日 | 2020-08-26 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.11 Å) | | 主引用文献 | Molecular basis for substrate recruitment to the PRMT5 methylosome.
Mol.Cell, 81, 2021
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7SER
 | | PRMT5/MEP50 with compound 30 bound | | 分子名称: | (2M)-2-{4-[4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl]-1-methyl-1H-pyrazol-5-yl}-1-benzothiophene-3-carbonitrile, 5'-DEOXY-5'-METHYLTHIOADENOSINE, Methylosome protein 50, ... | | 著者 | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Smith, C.R, Kulyk, S, Marx, M.A. | | 登録日 | 2021-10-01 | | 公開日 | 2022-01-26 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.14 Å) | | 主引用文献 | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers.
J.Med.Chem., 65, 2022
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7S1P
 | | PRMT5/MEP50 crystal structure with sinefungin bound | | 分子名称: | Methylosome protein 50, Protein arginine N-methyltransferase 5, SINEFUNGIN | | 著者 | Gunn, R.J, Thomas, N.C, Lawson, J.D, Ivetac, A, Kulyk, S, Smith, C.R, Marx, M.A. | | 登録日 | 2021-09-02 | | 公開日 | 2022-03-16 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.21 Å) | | 主引用文献 | Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers.
J.Med.Chem., 65, 2022
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6RLL
 | | CRYSTAL STRUCTURE OF THE HUMAN PRMT5:MEP50 COMPLEX with JNJ44064146 | | 分子名称: | (2~{R},3~{R},4~{S},5~{R})-2-(4-azanylpyrrolo[2,3-d]pyrimidin-7-yl)-5-(1,8-diazaspiro[4.5]decan-1-ylmethyl)oxolane-3,4-diol, Methylosome protein 50, Protein arginine N-methyltransferase 5 | | 著者 | Brown, D.G, Robinson, C.M, Pande, V. | | 登録日 | 2019-05-02 | | 公開日 | 2020-06-03 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.22 Å) | | 主引用文献 | A chemical probe for the methyl transferase PRMT5 with a novel
binding mode
To Be Published
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5EMJ
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5FA5
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4X60
 | | Crystal structure of PRMT5:MEP50 with EPZ015666 and sinefungin | | 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 (2.35 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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5C9Z
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5EMM
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5EML
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7ZVL
 | | HUMAN PRMT5:MEP50 Crystal Structure With MTA and Fragment Bound | | 分子名称: | 5'-DEOXY-5'-METHYLTHIOADENOSINE, CHLORIDE ION, GLYCEROL, ... | | 著者 | Ahmad, M.U, Koelmel, W, Arkhipova, V, Lawson, J.D, Smith, C.R, Gunn, R.J. | | 登録日 | 2022-05-16 | | 公開日 | 2022-10-19 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.39 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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7M05
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7MXG
 | | PRMT5(M420T mutant):MEP50 complexed with inhibitor PF-06855800 | | 分子名称: | 7-[(5R)-5-C-(4-chloro-3-fluorophenyl)-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine, Methylosome protein 50, Protein arginine N-methyltransferase 5 | | 著者 | McTigue, M, Deng, Y.L, Liu, W, Brooun, A. | | 登録日 | 2021-05-19 | | 公開日 | 2021-11-17 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.395 Å) | | 主引用文献 | SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance.
Mol.Cancer Ther., 21, 2022
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7MXC
 | | PRMT5:MEP50 complexed with adenosine | | 分子名称: | ADENOSINE, Methylosome protein 50, Protein arginine N-methyltransferase 5 | | 著者 | McTigue, M, Deng, Y.L, Liu, W, Brooun, A. | | 登録日 | 2021-05-18 | | 公開日 | 2021-11-17 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.41 Å) | | 主引用文献 | SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance.
Mol.Cancer Ther., 21, 2022
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7KIC
 | | PRMT5:MEP50 Complexed with 5,5-Bicyclic Inhibitor Compound 34 | | 分子名称: | (2R,3R,3aS,6S,6aR)-6-[(2-amino-3-bromoquinolin-7-yl)oxy]-2-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)hexahydro-3aH-cyclopenta[b]furan-3,3a-diol, 1,2-ETHANEDIOL, Methylosome protein 50, ... | | 著者 | Palte, R.L. | | 登録日 | 2020-10-23 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.43 Å) | | 主引用文献 | The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.
J.Med.Chem., 64, 2021
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