タイトル | The inhibition mechanism of human 20S proteasomes enables next-generation inhibitor design. |
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ジャーナル・号・ページ | Science, Vol. 353, Page 594-598, Year 2016 |
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掲載日 | 2016年6月29日 (構造データの登録日) |
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著者 | Schrader, J. / Henneberg, F. / Mata, R.A. / Tittmann, K. / Schneider, T.R. / Stark, H. / Bourenkov, G. / Chari, A. |
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リンク | Science / PubMed:27493187 |
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手法 | X線回折 |
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解像度 | 1.8 - 2.41 Å |
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構造データ | PDB-5le5: Native human 20S proteasome at 1.8 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 1.8 Å PDB-5lex: Native human 20S proteasome in Mg-Acetate at 2.2 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 2.2 Å PDB-5ley: Human 20S proteasome complex with Oprozomib at 1.9 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 1.9 Å PDB-5lez: Human 20S proteasome complex with Oprozomib in Mg-Acetate at 2.2 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 2.19 Å PDB-5lf0: Human 20S proteasome complex with Epoxomicin at 2.4 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 2.41 Å PDB-5lf1: Human 20S proteasome complex with Dihydroeponemycin at 2.0 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 2 Å PDB-5lf3: Human 20S proteasome complex with Bortezomib at 2.1 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 2.1 Å PDB-5lf4: Human 20S proteasome complex with Delanzomib at 2.0 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 1.99 Å PDB-5lf6: Human 20S proteasome complex with Z-LLY-ketoaldehyde at 2.1 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 2.07 Å PDB-5lf7: Human 20S proteasome complex with Ixazomib at 2.0 Angstrom 手法: X-RAY DIFFRACTION / 解像度: 2 Å |
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化合物 | ChemComp-6VC: ~{N}-[(2~{S})-1-[[(2~{S},3~{R},4~{S})-2,6-dimethyl-1,2,3-tris(oxidanyl)heptan-4-yl]amino]-3-oxidanyl-1-oxidanylidene-propan-2-yl]-6-methyl-heptanamide
ChemComp-BO2: N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE / ボルテゾミブ / 薬剤, 抗がん剤*YM
ChemComp-6V7: [(1~{R})-3-methyl-1-[[(2~{S},3~{S})-3-oxidanyl-2-[(6-phenylpyridin-2-yl)carbonylamino]butanoyl]amino]butyl]boronic acid
ChemComp-6V8: [(1~{R})-1-[2-[[2,5-bis(chloranyl)phenyl]carbonylamino]ethanoylamino]-3-methyl-butyl]boronic acid / イキサゾミブ
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由来 | - homo sapiens (ヒト)
- synthetic construct (人工物)
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キーワード | HYDROLASE / Proteasome / Multicatalytic Proteinase / NTN-Hydrolase |
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