タイトル | Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit. |
---|
ジャーナル・号・ページ | Biochem. J., Vol. 430, Page 461-476, Year 2010 |
---|
掲載日 | 2010年4月5日 (構造データの登録日) |
---|
著者 | Blackburn, C. / Gigstad, K.M. / Hales, P. / Garcia, K. / Jones, M. / Bruzzese, F.J. / Barrett, C. / Liu, J.X. / Soucy, T.A. / Sappal, D.S. ...Blackburn, C. / Gigstad, K.M. / Hales, P. / Garcia, K. / Jones, M. / Bruzzese, F.J. / Barrett, C. / Liu, J.X. / Soucy, T.A. / Sappal, D.S. / Bump, N. / Olhava, E.J. / Fleming, P. / Dick, L.R. / Tsu, C. / Sintchak, M.D. / Blank, J.L. |
---|
リンク | Biochem. J. / PubMed:20632995 |
---|
手法 | X線回折 |
---|
解像度 | 2.59 - 3.11 Å |
---|
構造データ | PDB-3mg0: Structure of yeast 20S proteasome with bortezomib 手法: X-RAY DIFFRACTION / 解像度: 2.68 Å PDB-3mg4: Structure of yeast 20S proteasome with Compound 1 手法: X-RAY DIFFRACTION / 解像度: 3.11 Å PDB-3mg6: Structure of yeast 20S open-gate proteasome with Compound 6 手法: X-RAY DIFFRACTION / 解像度: 2.6 Å PDB-3mg7: Structure of yeast 20S open-gate proteasome with Compound 8 手法: X-RAY DIFFRACTION / 解像度: 2.78 Å PDB-3mg8: Structure of yeast 20S open-gate proteasome with Compound 16 手法: X-RAY DIFFRACTION / 解像度: 2.59 Å |
---|
化合物 | 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-LXT: (2S)-2-amino-N-[(1S)-1-({(1S)-1-[(4-methylbenzyl)carbamoyl]-3-phenylpropyl}carbamoyl)-3-phenylpropyl]-4-phenylbutanamide
ChemComp-LZT: N~2~-{[(1S)-6-methoxy-3-oxo-2,3-dihydro-1H-inden-1-yl]acetyl}-N-{(1S)-1-[(4-methylbenzyl)carbamoyl]-3-phenylpropyl}-L-threoninamide
ChemComp-L2T: 4-(benzyloxy)-N-[(1S,2R)-2-hydroxy-1-({(1S)-1-[(2-methylbenzyl)carbamoyl]-3-phenylpropyl}carbamoyl)propyl]benzamide
ChemComp-L3T: N-(2,2-dimethylpropyl)-N~2~-[1H-indol-3-yl(oxo)acetyl]-L-asparaginyl-N-(2-methylbenzyl)-3-pyridin-4-yl-L-alaninamide
|
---|
由来 | ![](img/tx_yeast.gif) saccharomyces cerevisiae (パン酵母)
|
---|
キーワード | HYDROLASE / 20S proteasome |
---|