タイトル | Selective MCL-1 inhibitor ABBV-467 is efficacious in tumor models but is associated with cardiac troponin increases in patients. |
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ジャーナル・号・ページ | Commun Med (Lond), Vol. 3, Page 154-154, Year 2023 |
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掲載日 | 2022年9月22日 (構造データの登録日) |
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著者 | Yuda, J. / Will, C. / Phillips, D.C. / Abraham, L. / Alvey, C. / Avigdor, A. / Buck, W. / Besenhofer, L. / Boghaert, E. / Cheng, D. ...Yuda, J. / Will, C. / Phillips, D.C. / Abraham, L. / Alvey, C. / Avigdor, A. / Buck, W. / Besenhofer, L. / Boghaert, E. / Cheng, D. / Cojocari, D. / Doyle, K. / Hansen, T.M. / Huang, K. / Johnson, E.F. / Judd, A.S. / Judge, R.A. / Kalvass, J.C. / Kunzer, A. / Lam, L.T. / Li, R. / Martin, R.L. / Mastracchio, A. / Mitten, M. / Petrich, A. / Wang, J. / Ward, J.E. / Zhang, H. / Wang, X. / Wolff, J.E. / Bell-McGuinn, K.M. / Souers, A.J. |
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リンク | Commun Med (Lond) / PubMed:37880389 |
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手法 | X線回折 |
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解像度 | 1.55 - 2.406 Å |
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構造データ | PDB-8ekx: Structure of MBP-Mcl-1 in complex with MIK665 手法: X-RAY DIFFRACTION / 解像度: 1.55 Å PDB-8el0: Structure of MBP-Mcl-1 in complex with a macrocyclic compound 手法: X-RAY DIFFRACTION / 解像度: 1.917 Å PDB-8el1: Structure of MBP-Mcl-1 in complex with ABBV-467 手法: X-RAY DIFFRACTION / 解像度: 2.406 Å |
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化合物 | ChemComp-OK5: (2~{R})-2-[5-[3-chloranyl-2-methyl-4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]-6-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4-yl]oxy-3-[2-[[2-(2-methoxyphenyl)pyrimidin-4-yl]methoxy]phenyl]propanoic acid
ChemComp-WLW: (7R,20P)-18-chloro-1-(4-fluorophenyl)-10-{[(2M)-2-(2-methoxyphenyl)pyrimidin-4-yl]methoxy}-19-methyl-15-[2-(4-methylpiperazin-1-yl)ethyl]-7,8,15,16-tetrahydro-14H-17,20-etheno-9,13-(metheno)-6-oxa-2-thia-3,5,15-triazacyclooctadeca[1,2,3-cd]indene-7-carboxylic acid
ChemComp-WME: (7R,16R)-19,23-dichloro-10-{[2-(4-{[(2R)-1,4-dioxan-2-yl]methoxy}phenyl)pyrimidin-4-yl]methoxy}-1-(4-fluorophenyl)-20,22-dimethyl-16-[(4-methylpiperazin-1-yl)methyl]-7,8,15,16-tetrahydro-18,21-etheno-13,9-(metheno)-6,14,17-trioxa-2-thia-3,5-diazacyclononadeca[1,2,3-cd]indene-7-carboxylic acid
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由来 | ![](img/tx_bacteria.gif) escherichia coli k-12 (大腸菌) homo sapiens (ヒト)![](img/tx_bacteria.gif) escherichia coli (大腸菌)
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キーワード | APOPTOSIS / MBP-Mcl-1 fusion protein / MIK665 / inhibitor complex / ABBV-467 |
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