タイトル | DFG-out Mode of Inhibition by an Irreversible Type-1 Inhibitor Capable of Overcoming Gate-Keeper Mutations in FGF Receptors. |
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ジャーナル・号・ページ | Acs Chem. Biol., Vol. 10, Page 299-309, Year 2015 |
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掲載日 | 2014年6月26日 (構造データの登録日) |
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著者 | Huang, Z. / Tan, L. / Wang, H. / Liu, Y. / Blais, S. / Deng, J. / Neubert, T.A. / Gray, N.S. / Li, X. / Mohammadi, M. |
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リンク | Acs Chem. Biol. / PubMed:25317566 |
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手法 | X線回折 |
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解像度 | 1.501 - 2.203 Å |
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構造データ | PDB-4qq5: Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex With FIIN-2, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR Kinase Gate-Keeper Mutations 手法: X-RAY DIFFRACTION / 解像度: 2.203 Å PDB-4qqj: Crystal Structure of FGF Receptor (FGFR) 4 Kinase Domain Harboring the V550L Gate-Keeper Mutation 手法: X-RAY DIFFRACTION / 解像度: 1.682 Å PDB-4qqt: Crystal Structure of FGF Receptor (FGFR) 4 Tyrosine Kinase Domain 手法: X-RAY DIFFRACTION / 解像度: 1.501 Å PDB-4qrc: Crystal Structure of the Tyrosine Kinase Domain of FGF Receptor 4 in Complex with Ponatinib 手法: X-RAY DIFFRACTION / 解像度: 1.901 Å |
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化合物 | ChemComp-37O: N-(4-{[3-(3,5-dimethoxyphenyl)-7-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)propanamide
ChemComp-0LI: 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam / ポナチニブ / 薬剤*YM
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由来 | - homo sapiens (ヒト)
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キーワード | Transferase/transferase inhibitor / Kinase Domain Fold / Cell Signaling / Phosphotransferase / Plasmamembrane / Transferase-transferase inhibitor complex / TRANSFERASE |
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