6VHP
 
 | | Wild type EGFR in complex with LN2899 | | 分子名称: | Epidermal growth factor receptor, N-{3-[(4-{4-(4-fluorophenyl)-2-[(2-methoxyethyl)sulfanyl]-1H-imidazol-5-yl}pyridin-2-yl)amino]-4-methoxyphenyl}propanamide | | 著者 | Heppner, D.E, Eck, M.J. | | 登録日 | 2020-01-10 | | 公開日 | 2020-04-22 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (3.6 Å) | | 主引用文献 | Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.
J.Med.Chem., 63, 2020
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6VHN
 | | Wild type EGFR in complex with LN2057 | | 分子名称: | Epidermal growth factor receptor, N-[3-({4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl}amino)-4-methoxyphenyl]propanamide | | 著者 | Heppner, D.E, Eck, M.J. | | 登録日 | 2020-01-10 | | 公開日 | 2020-04-22 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.
J.Med.Chem., 63, 2020
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1U5D
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7M0Y
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Trametinib | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.45 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0Z
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and CH5126766 | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, N-(3-fluoro-4-{[4-methyl-2-oxo-7-(pyrimidin-2-yloxy)-2H-chromen-3-yl]methyl}pyridin-2-yl)-N'-methylsulfuric diamide, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.12 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0V
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Cobimetinib | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.16 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0W
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Pimasertib | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]pyridine-4-carboxamide, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.09 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0U
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Binimetinib | | 分子名称: | 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide, Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.09 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7M0T
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP and Selumetinib | | 分子名称: | 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide, Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Ha, B.H, Park, E, Eck, M.J. | | 登録日 | 2021-03-11 | | 公開日 | 2021-04-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.19 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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4LL0
 | | EGFR L858R/T790M in complex with PD168393 | | 分子名称: | Epidermal growth factor receptor, N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}propanamide | | 著者 | Yun, C.H, Eck, M.J. | | 登録日 | 2013-07-09 | | 公開日 | 2013-09-11 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (4 Å) | | 主引用文献 | Mechanism for activation of mutated epidermal growth factor receptors in lung cancer.
Proc.Natl.Acad.Sci.USA, 110, 2013
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6V2W
 | | Crystal structure of the BRAF:MEK1 kinases in complex with AMPPNP | | 分子名称: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Park, E, Eck, M.J. | | 登録日 | 2019-11-25 | | 公開日 | 2020-12-02 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (3.12 Å) | | 主引用文献 | Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7MYX
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7JXQ
 | | EGFR kinase (T790M/V948R) in complex with allosteric inhibitor JBJ-09-063 | | 分子名称: | (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-{6-[4-(1-methylpiperidin-4-yl)phenyl]-1-oxo-1,3-dihydro-2H-isoindol-2-yl}-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Beyett, T.S, Eck, M.J. | | 登録日 | 2020-08-27 | | 公開日 | 2021-09-08 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | | 主引用文献 | An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer.
Nat Cancer, 3, 2022
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7JXH
 | | HER2 in complex with JBJ-08-178-01 | | 分子名称: | (2E)-N-[3-cyano-7-ethoxy-4-({3-methyl-4-[([1,2,4]triazolo[1,5-a]pyridin-7-yl)oxy]phenyl}amino)quinolin-6-yl]-4-(dimethylamino)but-2-enamide, Receptor tyrosine-protein kinase erbB-2 | | 著者 | Beyett, T.S, Eck, M.J. | | 登録日 | 2020-08-27 | | 公開日 | 2021-09-08 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.27 Å) | | 主引用文献 | A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non-Small Cell Lung Cancer.
Cancer Res., 82, 2022
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2F31
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2CBL
 | | N-TERMINAL DOMAIN OF CBL IN COMPLEX WITH ITS BINDING SITE ON ZAP-70 | | 分子名称: | CALCIUM ION, PROTO-ONCOGENE CBL, ZAP-70 | | 著者 | Meng, W, Sawasdikosol, S, Burakoff, S.J, Eck, M.J. | | 登録日 | 1998-08-28 | | 公開日 | 1999-05-18 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Structure of the amino-terminal domain of Cbl complexed to its binding site on ZAP-70 kinase.
Nature, 398, 1999
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1EG3
 | | STRUCTURE OF A DYSTROPHIN WW DOMAIN FRAGMENT IN COMPLEX WITH A BETA-DYSTROGLYCAN PEPTIDE | | 分子名称: | DYSTROPHIN | | 著者 | Huang, X, Poy, F, Zhang, R, Joachimiak, A, Sudol, M, Eck, M.J. | | 登録日 | 2000-02-11 | | 公開日 | 2000-08-23 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structure of a WW domain containing fragment of dystrophin in complex with beta-dystroglycan.
Nat.Struct.Biol., 7, 2000
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1EG4
 | | STRUCTURE OF A DYSTROPHIN WW DOMAIN FRAGMENT IN COMPLEX WITH A BETA-DYSTROGLYCAN PEPTIDE | | 分子名称: | BETA-DYSTROGLYCAN, DYSTROPHIN | | 著者 | Huang, X, Poy, F, Zhang, R, Joachimiak, A, Sudol, M, Eck, M.J. | | 登録日 | 2000-02-11 | | 公開日 | 2000-08-23 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structure of a WW domain containing fragment of dystrophin in complex with beta-dystroglycan.
Nat.Struct.Biol., 7, 2000
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2OTX
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6V34
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2SHP
 | | TYROSINE PHOSPHATASE SHP-2 | | 分子名称: | DODECANE-TRIMETHYLAMINE, SHP-2 | | 著者 | Hof, P, Pluskey, S, Dhe-Paganon, S, Eck, M.J, Shoelson, S.E. | | 登録日 | 1997-12-01 | | 公開日 | 1999-02-16 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Crystal structure of the tyrosine phosphatase SHP-2.
Cell(Cambridge,Mass.), 92, 1998
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1UX4
 | | Crystal structures of a Formin Homology-2 domain reveal a tethered-dimer architecture | | 分子名称: | BNI1 PROTEIN | | 著者 | Xu, Y, Moseley, J.B, Sagot, I, Poy, F, Pellman, D, Goode, B.L, Eck, M.J. | | 登録日 | 2004-02-19 | | 公開日 | 2004-03-11 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Crystal Structures of a Formin Homology-2 Domain Reveal a Tethered Dimer Architecture
Cell(Cambridge,Mass.), 116, 2004
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7KXZ
 | | Active conformation of EGFR kinase in complex with BI-4020 | | 分子名称: | (20R)-10,15,20-trimethyl-2-[(4-methylpiperazin-1-yl)methyl]-18,19,20,21-tetrahydro-15H,17H-12,8-(metheno)pyrazolo[3',4':2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-7(6H)-one, CHLORIDE ION, Epidermal growth factor receptor | | 著者 | Beyett, T.S, Eck, M.J. | | 登録日 | 2020-12-06 | | 公開日 | 2022-01-19 | | 最終更新日 | 2024-05-29 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structural Analysis of the Macrocyclic Inhibitor BI-4020 Binding to EGFR Kinase.
Chemmedchem, 2024
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1U5E
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7KY0
 | | Inactive conformation of EGFR (T790M/V948R) kinase in complex with BI-4020 | | 分子名称: | (20R)-10,15,20-trimethyl-2-[(4-methylpiperazin-1-yl)methyl]-18,19,20,21-tetrahydro-15H,17H-12,8-(metheno)pyrazolo[3',4':2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-7(6H)-one, Epidermal growth factor receptor | | 著者 | Beyett, T.S, Eck, M.J. | | 登録日 | 2020-12-06 | | 公開日 | 2022-01-19 | | 最終更新日 | 2024-05-29 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Structural Analysis of the Macrocyclic Inhibitor BI-4020 Binding to EGFR Kinase.
Chemmedchem, 2024
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