タイトル | Structural and biochemical evaluation of bisubstrate inhibitors of protein arginine N-methyltransferases PRMT1 and CARM1 (PRMT4). |
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ジャーナル・号・ページ | Biochem. J., Vol. 477, Page 787-800, Year 2020 |
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掲載日 | 2019年7月4日 (構造データの登録日) |
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著者 | Gunnell, E.A. / Al-Noori, A. / Muhsen, U. / Davies, C.C. / Dowden, J. / Dreveny, I. |
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リンク | Biochem. J. / PubMed:32011657 |
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手法 | X線回折 |
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解像度 | 1.86 - 2.659 Å |
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構造データ | PDB-6s70: Crystal structure of CARM1 in complex with inhibitor UM251 手法: X-RAY DIFFRACTION / 解像度: 2.3 Å PDB-6s71: Crystal structure of CARM1 in complex with inhibitor WH5C 手法: X-RAY DIFFRACTION / 解像度: 2.062 Å PDB-6s74: Crystal structure of CARM1 in complex with inhibitor UM305 手法: X-RAY DIFFRACTION / 解像度: 2.1 Å PDB-6s77: Crystal structure of CARM1 N265Y mutant in complex with inhibitor AA183 手法: X-RAY DIFFRACTION / 解像度: 2.12 Å PDB-6s79: Crystal structure of CARM1 in complex with inhibitor AA183 手法: X-RAY DIFFRACTION / 解像度: 2.1 Å PDB-6s7a: Crystal structure of CARM1 in complex with inhibitor AA175 手法: X-RAY DIFFRACTION / 解像度: 1.86 Å PDB-6s7b: Crystal structure of CARM1 in complex with inhibitor UM249 手法: X-RAY DIFFRACTION / 解像度: 2.659 Å PDB-6s7c: Crystal structure of CARM1 in complex with inhibitor UM079 手法: X-RAY DIFFRACTION / 解像度: 2.3 Å |
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化合物 | ChemComp-KYB: 1-[5-[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl-(3-azanylpropyl)amino]pentyl]guanidine
ChemComp-KYE: (2~{S})-4-[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl-(5-carbamimidamidopentyl)amino]-2-azanyl-butanoic acid
ChemComp-KY8: (2~{R},3~{R},4~{S},5~{R})-2-(6-aminopurin-9-yl)-5-[[3-azanylpropyl-[3-(pyrimidin-2-ylamino)propyl]amino]methyl]oxolane-3,4-diol
ChemComp-KXW: (2~{S})-4-[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl-[3-(pyridin-2-ylamino)propyl]amino]-2-azanyl-butanoic acid
ChemComp-KY5: (2~{R},3~{R},4~{S},5~{R})-2-(6-aminopurin-9-yl)-5-[[3-azanylpropyl-[3-(pyridin-2-ylamino)propyl]amino]methyl]oxolane-3,4-diol
ChemComp-KYH: 1-[4-[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl-(3-azanylpropyl)amino]butyl]guanidine
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由来 | homo sapiens (ヒト)
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キーワード | TRANSFERASE / Inhibitor / Complex / Arginine methyltransferase |
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