タイトル | Biochemical analysis of EGFR exon20 insertion variants insASV and insSVD and their inhibitor sensitivity. |
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ジャーナル・号・ページ | Proc. Natl. Acad. Sci. USA, Vol. 121, Page e2417144121-e2417144121, Year 2024 |
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掲載日 | 2022年11月5日 (構造データの登録日) |
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著者 | Zhao, H. / Beyett, T.S. / Jiang, J. / Rana, J.K. / Schaeffner, I.K. / Santana, J. / Janne, P.A. / Eck, M.J. |
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リンク | Proc. Natl. Acad. Sci. USA / PubMed:39471218 |
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手法 | X線回折 |
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解像度 | 2.3 - 3.2 Å |
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構造データ | PDB-8f1h: EGFR kinase in complex with TAS6417 (CLN-081) 手法: X-RAY DIFFRACTION / 解像度: 2.8 Å PDB-8f1w: EGFR(T790M/V948R) kinase in complex with poziotinib 手法: X-RAY DIFFRACTION / 解像度: 3.2 Å PDB-8f1x: EGFR kinase in complex with mobocertinib (TAK-788) 手法: X-RAY DIFFRACTION / 解像度: 2.3 Å PDB-8f1y: EGFR kinase in complex with poziotinib 手法: X-RAY DIFFRACTION / 解像度: 2.75 Å PDB-8f1z: EGFR kinase in complex with Bayer #33 手法: X-RAY DIFFRACTION / 解像度: 2.4 Å |
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化合物 | ChemComp-X9H: N-[(5P,8S,10R)-4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl]prop-2-enamide
ChemComp-R2E: 1-[4-[4-[[3,4-bis(chloranyl)-2-fluoranyl-phenyl]amino]-7-methoxy-quinazolin-6-yl]oxypiperidin-1-yl]propan-1-one
ChemComp-R28: propan-2-yl 2-[[4-[2-(dimethylamino)ethyl-methyl-amino]-2-methoxy-5-(propanoylamino)phenyl]amino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate / 阻害剤*YM
ChemComp-X9B: (2P)-3-(3-chloro-2-methoxyanilino)-2-[3-(2-methoxy-2-methylpropoxy)pyridin-4-yl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
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由来 | - homo sapiens (ヒト)
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キーワード | TRANSFERASE/TRANSFERASE INHIBITOR / EGFR / kinase / exon 20 / inhibitor / TRANSFERASE / TRANSFERASE-TRANSFERASE INHIBITOR complex |
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