タイトル | Structural basis for the action of the drug trametinib at KSR-bound MEK. |
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ジャーナル・号・ページ | Nature, Vol. 588, Page 509-514, Year 2020 |
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掲載日 | 2020年8月20日 (構造データの登録日) |
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著者 | Khan, Z.M. / Real, A.M. / Marsiglia, W.M. / Chow, A. / Duffy, M.E. / Yerabolu, J.R. / Scopton, A.P. / Dar, A.C. |
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リンク | Nature / PubMed:32927473 |
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手法 | X線回折 |
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解像度 | 2.82 - 3.63 Å |
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構造データ | PDB-7juq: Crystal Structure of KSR2:MEK1 in complex with ADP 手法: X-RAY DIFFRACTION / 解像度: 3.22 Å PDB-7jur: Crystal Structure of KSR2:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor Trametinib 手法: X-RAY DIFFRACTION / 解像度: 2.82 Å PDB-7jus: Crystal Structure of KSR2:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor Cobimetinib 手法: X-RAY DIFFRACTION / 解像度: 2.99 Å PDB-7jut: Crystal Structure of KSR2:MEK1 in complex with ANP-PNP, and allosteric MEK inhibitor Selumetinib 手法: X-RAY DIFFRACTION / 解像度: 3.09 Å PDB-7juu: Crystal Structure of KSR2:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor PD0325901 手法: X-RAY DIFFRACTION / 解像度: 3.19 Å PDB-7juv: Crystal Structure of KSR2:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor APS-9-95-1 手法: X-RAY DIFFRACTION / 解像度: 3.36 Å PDB-7juw: Crystal Structure of KSR1:MEK1 in complex with AMP-PNP 手法: X-RAY DIFFRACTION / 解像度: 2.88 Å PDB-7jux: Crystal Structure of KSR1:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor Trametinib 手法: X-RAY DIFFRACTION / 解像度: 3.34 Å PDB-7juy: Crystal Structure of KSR1:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor Cobimetinib 手法: X-RAY DIFFRACTION / 解像度: 3.096 Å PDB-7juz: Crystal Structure of KSR1:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor Selumetinib 手法: X-RAY DIFFRACTION / 解像度: 3.21 Å PDB-7jv0: Crystal Structure of KSR1:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor PD0325901 手法: X-RAY DIFFRACTION / 解像度: 3.63 Å PDB-7jv1: Crystal Structure of KSR1:MEK1 in complex with AMP-PNP, and allosteric MEK inhibitor APS-9-95-1 手法: X-RAY DIFFRACTION / 解像度: 3.62 Å |
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化合物 | ChemComp-ANP: PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER / AMP-PNP / AMP-PNP, エネルギー貯蔵分子類似体*YM
ChemComp-3EW: 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide / AZD-6244 / 薬剤*YM
ChemComp-4BM: N-{[(2R)-2,3-dihydroxypropyl]oxy}-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide / PD-0325901
ChemComp-VKG: N-(3-{3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)-N'-methylsulfuric diamide
ChemComp-EUI: [3,4-BIS(FLUORANYL)-2-[(2-FLUORANYL-4-IODANYL-PHENYL)AMINO]PHENYL]-[3-OXIDANYL-3-[(2S)-PIPERIDIN-2-YL]AZETIDIN-1-YL]METHANONE / コビメチニブ / 薬剤, 抗がん剤, 阻害剤*YM
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由来 | homo sapiens (ヒト)![](img/tx_mammal.gif) oryctolagus cuniculus (ウサギ)
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キーワード | TRANSFERASE/TRANSFERASE INHIBITOR / Kinase / Pseudokinase / drug target / cell signaling and cancer / TRANSFERASE / TRANSFERASE-TRANSFERASE INHIBITOR complex / cell signaling / cancer |
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