タイトル | Hijacking DNA methyltransferase transition state analogues to produce chemical scaffolds for PRMT inhibitors. |
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ジャーナル・号・ページ | Philos. Trans. R. Soc. Lond. B Biol. Sci., Vol. 373, Year 2018 |
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掲載日 | 2016年9月12日 (構造データの登録日) |
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著者 | Halby, L. / Marechal, N. / Pechalrieu, D. / Cura, V. / Franchini, D.M. / Faux, C. / Alby, F. / Troffer-Charlier, N. / Kudithipudi, S. / Jeltsch, A. ...Halby, L. / Marechal, N. / Pechalrieu, D. / Cura, V. / Franchini, D.M. / Faux, C. / Alby, F. / Troffer-Charlier, N. / Kudithipudi, S. / Jeltsch, A. / Aouadi, W. / Decroly, E. / Guillemot, J.C. / Page, P. / Ferroud, C. / Bonnefond, L. / Guianvarc'h, D. / Cavarelli, J. / Arimondo, P.B. |
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リンク | Philos. Trans. R. Soc. Lond. B Biol. Sci. / PubMed:29685976 |
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手法 | X線回折 |
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解像度 | 1.66 - 2.341 Å |
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構造データ | PDB-5lv2: Crystal structure of mouse CARM1 in complex with inhibitor LH1246 手法: X-RAY DIFFRACTION / 解像度: 2.29 Å PDB-5lv3: Crystal structure of mouse CARM1 in complex with ligand LH1561Br 手法: X-RAY DIFFRACTION / 解像度: 1.8 Å PDB-5lv4: Crystal structure of mouse PRMT6 in complex with inhibitor LH1236 手法: X-RAY DIFFRACTION / 解像度: 1.66 Å PDB-5lv5: Crystal structure of mouse PRMT6 in complex with inhibitor LH1458 手法: X-RAY DIFFRACTION / 解像度: 1.802 Å PDB-5tbh: Crystal structure of mouse CARM1 in complex with inhibitor LH1236 手法: X-RAY DIFFRACTION / 解像度: 2.341 Å PDB-5tbi: Crystal structure of mouse CARM1 in complex with inhibitor LH1427 手法: X-RAY DIFFRACTION / 解像度: 2.294 Å PDB-5tbj: Crystal structure of mouse CARM1 in complex with inhibitor LH1452 手法: X-RAY DIFFRACTION / 解像度: 2.32 Å |
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化合物 | ChemComp-SAO: 5'-S-[(3S)-3-azaniumyl-3-carboxypropyl]-5'-thioadenosine
ChemComp-LHB: 5-[[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methylamino]methyl]-4-azanyl-1-(methoxymethyl)pyrimidin-2-one
ChemComp-LHF: 5-[[2-[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]ethylamino]methyl]-4-azanyl-1-[2-(4-bromanylphenoxy)ethyl]pyrimidin-2-one
ChemComp-78K: (2~{R})-4-[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl-[[4-azanyl-1-(methoxymethyl)-2-oxidanylidene-pyrimidin-5-yl]methyl]amino]-2-azanyl-butanoic acid
ChemComp-78G: 2-[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]ethyl-[[4-azanyl-1-(methoxymethyl)-2-oxidanylidene-pyrimidin-5-yl]methyl]-[(3~{S})-3-azanyl-4-oxidanyl-4-oxidanylidene-butyl]azanium
ChemComp-78V: 4-[2-[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methylamino]ethylamino]-1-(methoxymethyl)pyrimidin-2-one
ChemComp-LHD: 2-[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]ethyl-[[4-azanyl-1-(methoxymethyl)-2-oxidanylidene-pyrimidin-5-yl]methyl]azanium
ChemComp-PG6: 1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE / ペンタグリム
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由来 | ![](img/tx_mammal.gif) mus musculus (ハツカネズミ)
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キーワード | TRANSFERASE / PROTEIN ARGININE METHYLTRANSFERASE / CATALYTIC DOMAIN / CHROMATIN REGULATOR / MRNA PROCESSING / MRNA SPLICING / NUCLEUS / S-ADENOSYL-L-METHIONINE / TRANSCRIPTION / TRANSCRIPTION REGULATION |
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