タイトル | Enzyme inhibition by hydroamination: design and mechanism of a hybrid carmaphycin-syringolin enone proteasome inhibitor. |
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ジャーナル・号・ページ | Chem. Biol., Vol. 21, Page 782-791, Year 2014 |
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掲載日 | 2012年10月20日 (構造データの登録日) |
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著者 | Trivella, D.B. / Pereira, A.R. / Stein, M.L. / Kasai, Y. / Byrum, T. / Valeriote, F.A. / Tantillo, D.J. / Groll, M. / Gerwick, W.H. / Moore, B.S. |
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リンク | Chem. Biol. / PubMed:24930969 |
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手法 | X線回折 |
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解像度 | 2.5 - 2.8 Å |
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構造データ | PDB-4hnp: Crystal structure of yeast 20S proteasome in complex with vinylketone carmaphycin analogue VNK1 手法: X-RAY DIFFRACTION / 解像度: 2.8 Å PDB-4hrc: Crystal structure of yeast 20S proteasome in complex with epoxyketone carmaphycin analogue 3 手法: X-RAY DIFFRACTION / 解像度: 2.8 Å PDB-4hrd: Crystal structure of yeast 20S proteasome in complex with the natural product carmaphycin A 手法: X-RAY DIFFRACTION / 解像度: 2.8 Å PDB-4ltc: Crystal structure of yeast 20S proteasome in complex with enone carmaphycin analogue 6 手法: X-RAY DIFFRACTION / 解像度: 2.5 Å |
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化合物 | ChemComp-ONK: N-hexanoyl-L-valyl-N~1~-[(3S,4S)-3-hydroxy-2,6-dimethylhept-1-en-4-yl]-N~5~,N~5~-dimethyl-L-glutamamide
ChemComp-VNK: N-hexanoyl-L-valyl-N~1~-[(3S,4S)-3-hydroxy-2,6-dimethylheptan-4-yl]-N~5~,N~5~-dimethyl-L-glutamamide
ChemComp-OV2: N-hexanoyl-L-valyl-N~1~-[(2R,3S,4S)-1,3-dihydroxy-2,6-dimethylheptan-4-yl]-N~5~,N~5~-dimethyl-L-glutamamide
ChemComp-OV1: N-[(2S)-1-({(2S)-1-{[(2R,3S,4S)-1,3-dihydroxy-2,6-dimethylheptan-4-yl]amino}-4-[(R)-methylsulfinyl]-1-oxobutan-2-yl}amino)-3-methyl-1-oxobutan-2-yl]hexanamide
ChemComp-EC6: N-hexanoyl-L-valyl-N~1~-[(4S,5S,6R)-5-hydroxy-2,6-dimethyloctan-4-yl]-N~5~,N~5~-dimethyl-L-glutamamide
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由来 | - saccharomyces cerevisiae s288c (パン酵母)
- saccharomyces cerevisiae (パン酵母)
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キーワード | HYDROLASE/HYDROLASE INHIBITOR / proteasome / inhibitor / carmaphycin / epoxyketone / vinylketone / HYDROLASE / HYDROLASE-HYDROLASE INHIBITOR complex |
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