タイトル | The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models. |
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ジャーナル・号・ページ | Nature, Vol. 538, Page 477-482, Year 2016 |
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掲載日 | 2016年8月9日 (構造データの登録日) |
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著者 | Kotschy, A. / Szlavik, Z. / Murray, J. / Davidson, J. / Maragno, A.L. / Le Toumelin-Braizat, G. / Chanrion, M. / Kelly, G.L. / Gong, J.N. / Moujalled, D.M. ...Kotschy, A. / Szlavik, Z. / Murray, J. / Davidson, J. / Maragno, A.L. / Le Toumelin-Braizat, G. / Chanrion, M. / Kelly, G.L. / Gong, J.N. / Moujalled, D.M. / Bruno, A. / Csekei, M. / Paczal, A. / Szabo, Z.B. / Sipos, S. / Radics, G. / Proszenyak, A. / Balint, B. / Ondi, L. / Blasko, G. / Robertson, A. / Surgenor, A. / Dokurno, P. / Chen, I. / Matassova, N. / Smith, J. / Pedder, C. / Graham, C. / Studeny, A. / Lysiak-Auvity, G. / Girard, A.M. / Grave, F. / Segal, D. / Riffkin, C.D. / Pomilio, G. / Galbraith, L.C. / Aubrey, B.J. / Brennan, M.S. / Herold, M.J. / Chang, C. / Guasconi, G. / Cauquil, N. / Melchiore, F. / Guigal-Stephan, N. / Lockhart, B. / Colland, F. / Hickman, J.A. / Roberts, A.W. / Huang, D.C. / Wei, A.H. / Strasser, A. / Lessene, G. / Geneste, O. |
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リンク | Nature / PubMed:27760111 |
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手法 | X線回折 |
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解像度 | 2.2 Å |
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構造データ | PDB-5lof: Crystal structure of the MBP-MCL1 complex with highly selective and potent inhibitor of MCL1 手法: X-RAY DIFFRACTION / 解像度: 2.2 Å |
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化合物 | ChemComp-70R: (2~{R})-2-[5-[3-chloranyl-2-methyl-4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]-6-(5-fluoranylfuran-2-yl)thieno[2,3-d]pyrimidin-4-yl]oxy-3-[2-[[2-[2,2,2-tris(fluoranyl)ethyl]pyrazol-3-yl]methoxy]phenyl]propanoic acid / S-63845
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由来 | - escherichia coli o157:h7 (大腸菌)
- homo sapiens (ヒト)
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キーワード | APOPTOSIS/INHIBITOR / APOPTOSIS-INHIBITOR COMPLEX / MCL-1 / S S63845 / MBP |
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