タイトル | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation. |
---|
ジャーナル・号・ページ | Proc. Natl. Acad. Sci. USA, Vol. 118, Year 2021 |
---|
掲載日 | 2019年11月25日 (構造データの登録日) |
---|
著者 | Gonzalez-Del Pino, G.L. / Li, K. / Park, E. / Schmoker, A.M. / Ha, B.H. / Eck, M.J. |
---|
リンク | Proc. Natl. Acad. Sci. USA / PubMed:34470822 |
---|
手法 | X線回折 |
---|
解像度 | 2.47 - 3.45 Å |
---|
構造データ | PDB-6v2w: Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP 手法: X-RAY DIFFRACTION / 解像度: 3.12 Å PDB-7m0t: Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Selumetinib 手法: X-RAY DIFFRACTION / 解像度: 3.19 Å PDB-7m0u: Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Binimetinib 手法: X-RAY DIFFRACTION / 解像度: 3.09 Å PDB-7m0v: Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Cobimetinib 手法: X-RAY DIFFRACTION / 解像度: 3.16 Å PDB-7m0w: Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Pimasertib 手法: X-RAY DIFFRACTION / 解像度: 3.09 Å PDB-7m0x: Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and PD0325901 手法: X-RAY DIFFRACTION / 解像度: 2.47 Å PDB-7m0y: Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Trametinib 手法: X-RAY DIFFRACTION / 解像度: 3.45 Å PDB-7m0z: Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and CH5126766 手法: X-RAY DIFFRACTION / 解像度: 3.12 Å |
---|
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-QO7: 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide / ビニメチニブ / 薬剤, 抗がん剤, 阻害剤*YM
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
ChemComp-QOA: N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]pyridine-4-carboxamide / ピマセルチブ
ChemComp-4BM: N-{[(2R)-2,3-dihydroxypropyl]oxy}-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide / PD-0325901
ChemComp-CHU: N-(3-fluoro-4-{[4-methyl-2-oxo-7-(pyrimidin-2-yloxy)-2H-chromen-3-yl]methyl}pyridin-2-yl)-N'-methylsulfuric diamide / CH-5126766
|
---|
由来 | homo sapiens (ヒト)
|
---|
キーワード | TRANSFERASE / BRAF / MEK1 |
---|