4R3P
 
 | | Crystal structures of EGFR in complex with Mig6 | | 分子名称: | Epidermal growth factor receptor, peptide from ERBB receptor feedback inhibitor 1 | | 著者 | Park, E, Kim, N, Yi, Z, Cho, A, Kim, K, Ficarro, S.B, Park, A, Park, W.Y, Murray, B, Meyerson, M, Beroukim, R, Marto, J.A, Cho, J, Eck, M.J. | | 登録日 | 2014-08-17 | | 公開日 | 2015-08-12 | | 最終更新日 | 2015-09-16 | | 実験手法 | X-RAY DIFFRACTION (2.905 Å) | | 主引用文献 | Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6.
Nat.Struct.Mol.Biol., 22, 2015
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1JPW
 | | Crystal Structure of a Human Tcf-4 / beta-Catenin Complex | | 分子名称: | BETA-CATENIN, transcription factor 7-like 2 | | 著者 | Poy, F, Lepourcelet, M, Shivdasani, R.A, Eck, M.J. | | 登録日 | 2001-08-03 | | 公開日 | 2001-12-05 | | 最終更新日 | 2023-08-16 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Structure of a human Tcf4-beta-catenin complex.
Nat.Struct.Biol., 8, 2001
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6P1D
 | | Crystal structure of EGFR with mutant-selective dihydrodibenzodiazepinone allosteric inhibitor | | 分子名称: | 10-benzyl-8-fluoro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Heppner, D.E, Eck, M.J. | | 登録日 | 2019-05-19 | | 公開日 | 2019-12-18 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Acs Med.Chem.Lett., 10, 2019
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6P8Q
 | | EGFR in complex with a dihydrodibenzodiazepinone allosteric inhibitor. | | 分子名称: | 1,2-ETHANEDIOL, 10-benzyl-2-fluoro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one, ADENOSINE MONOPHOSPHATE, ... | | 著者 | Yun, C.H, Heppner, D.E, Eck, M.J. | | 登録日 | 2019-06-07 | | 公開日 | 2019-12-18 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Acs Med.Chem.Lett., 10, 2019
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2ITO
 | | Crystal structure of EGFR kinase domain G719S mutation in complex with Iressa | | 分子名称: | EPIDERMAL GROWTH FACTOR RECEPTOR, Gefitinib | | 著者 | Yun, C.-H, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | 登録日 | 2006-05-25 | | 公開日 | 2007-04-03 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (3.25 Å) | | 主引用文献 | Structures of Lung Cancer-Derived Egfr Mutants and Inhibitor Complexes: Mechanism of Activation and Insights Into Differential Inhibitor Sensitivity
Cancer Cell, 11, 2007
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6PP9
 | | Crystal structure of BRAF:MEK1 complex | | 分子名称: | 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide, CHLORIDE ION, Dual specificity mitogen-activated protein kinase kinase 1, ... | | 著者 | Li, K, Gonzalez Del-Pino, G, Park, E, Eck, M.J. | | 登録日 | 2019-07-05 | | 公開日 | 2019-10-09 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.59 Å) | | 主引用文献 | Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes.
Nature, 575, 2019
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6Q0J
 | | Structure of a MAPK pathway complex | | 分子名称: | 14-3-3 protein zeta, 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide, Dual specificity mitogen-activated protein kinase kinase 1, ... | | 著者 | Park, E, Rawson, S, Jeon, H, Eck, M.J. | | 登録日 | 2019-08-01 | | 公開日 | 2019-10-09 | | 最終更新日 | 2020-04-22 | | 実験手法 | ELECTRON MICROSCOPY (4.9 Å) | | 主引用文献 | Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes.
Nature, 575, 2019
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6Q0K
 | | Structure of a MAPK pathway complex | | 分子名称: | 14-3-3 protein zeta/delta, Serine/threonine-protein kinase B-raf | | 著者 | Park, E, Rawson, S, Jeon, H, Eck, M.J. | | 登録日 | 2019-08-01 | | 公開日 | 2019-10-09 | | 最終更新日 | 2020-04-22 | | 実験手法 | ELECTRON MICROSCOPY (6.8 Å) | | 主引用文献 | Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes.
Nature, 575, 2019
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2IUH
 | | Crystal structure of the PI3-kinase p85 N-terminal SH2 domain in complex with c-Kit phosphotyrosyl peptide | | 分子名称: | C-KIT PHOSPHOTYROSYL PEPTIDE, PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY ALPHA SUBUNIT | | 著者 | Nolte, R.T, Eck, M.J, Schlessinger, J, Shoelson, S.E, Harrison, S.C. | | 登録日 | 2006-06-03 | | 公開日 | 2006-06-06 | | 最終更新日 | 2021-04-28 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Crystal Structure of the Pi 3-Kinase P85 Amino-Terminal Sh2 Domain and its Phosphopeptide Complexes
Nat.Struct.Biol., 3, 1996
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2IUG
 | | Crystal structure of the PI3-kinase p85 N-terminal SH2 domain | | 分子名称: | PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY ALPHA SUBUNIT | | 著者 | Nolte, R.T, Eck, M.J, Schlessinger, J, Shoelson, S.E, Harrison, S.C. | | 登録日 | 2006-06-03 | | 公開日 | 2006-06-06 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.89 Å) | | 主引用文献 | Crystal Structure of the Pi 3-Kinase P85 Amino-Terminal Sh2 Domain and its Phosphopeptide Complexes
Nat.Struct.Biol., 3, 1996
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2IUI
 | | Crystal structure of the PI3-kinase p85 N-terminal SH2 domain in complex with PDGFR phosphotyrosyl peptide | | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Platelet-derived growth factor receptor beta | | 著者 | Nolte, R.T, Eck, M.J, Schlessinger, J, Shoelson, S.E, Harrison, S.C. | | 登録日 | 2006-06-03 | | 公開日 | 2006-06-06 | | 最終更新日 | 2021-04-28 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Crystal Structure of the Pi 3-Kinase P85 Amino- Terminal Sh2 Domain and its Phosphopeptide Complexes
Nat.Struct.Biol., 3, 1996
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6WXN
 | | EGFR(T790M/V948R) in complex with LN3844 | | 分子名称: | CHLORIDE ION, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Heppner, D.E, Eck, M.J. | | 登録日 | 2020-05-11 | | 公開日 | 2021-05-19 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.76 Å) | | 主引用文献 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.
J.Med.Chem., 65, 2022
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8GK5
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8GB4
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6XL4
 | | EGFR(T790M/V948R) in complex with AZD9291 and DDC4002 | | 分子名称: | 10-benzyl-8-fluoro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Heppner, D.E, Beyett, T.S, Eck, M.J. | | 登録日 | 2020-06-28 | | 公開日 | 2021-06-30 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.06 Å) | | 主引用文献 | Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors.
Nat Commun, 13, 2022
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4WD5
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4IM3
 | | Structure of Tank-Binding Kinase 1 | | 分子名称: | CHLORIDE ION, MERCURY (II) ION, N-(3-{[5-iodo-4-({3-[(thiophen-2-ylcarbonyl)amino]propyl}amino)pyrimidin-2-yl]amino}phenyl)pyrrolidine-1-carboxamide, ... | | 著者 | Tu, D, Eck, M.J. | | 登録日 | 2013-01-01 | | 公開日 | 2013-03-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (3.342 Å) | | 主引用文献 | Structure and ubiquitination-dependent activation of TANK-binding kinase 1.
Cell Rep, 3, 2013
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4IM2
 | | Structure of Tank-Binding Kinase 1 | | 分子名称: | CHLORIDE ION, N-(3-{[5-iodo-4-({3-[(thiophen-2-ylcarbonyl)amino]propyl}amino)pyrimidin-2-yl]amino}phenyl)pyrrolidine-1-carboxamide, Serine/threonine-protein kinase TBK1 | | 著者 | Tu, D, Eck, M.J. | | 登録日 | 2013-01-01 | | 公開日 | 2013-03-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.5001 Å) | | 主引用文献 | Structure and ubiquitination-dependent activation of TANK-binding kinase 1.
Cell Rep, 3, 2013
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4IM0
 | | Structure of Tank-Binding Kinase 1 | | 分子名称: | N-{3-[(5-cyclopropyl-2-{[3-(morpholin-4-ylmethyl)phenyl]amino}pyrimidin-4-yl)amino]propyl}cyclobutanecarboxamide, Serine/threonine-protein kinase TBK1 | | 著者 | Tu, D, Eck, M.J. | | 登録日 | 2013-01-01 | | 公開日 | 2013-03-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.4001 Å) | | 主引用文献 | Structure and ubiquitination-dependent activation of TANK-binding kinase 1.
Cell Rep, 3, 2013
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8TJL
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7U99
 | | EGFR kinase in complex with a macrocyclic inhibitor | | 分子名称: | 19-chloro-22-methoxy-8,9,11,12,14,15-hexahydro-21H-4,6-ethenopyrimido[5,4-m][1,4,7,10,15]benzotetraoxazacycloheptadecine, CITRATE ANION, Epidermal growth factor receptor | | 著者 | Beyett, T.S, Eck, M.J. | | 登録日 | 2022-03-10 | | 公開日 | 2022-11-23 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
J.Med.Chem., 65, 2022
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7U98
 | | EGFR(T790M/V948R) in complex with a macrocyclic inhibitor | | 分子名称: | 19-chloro-18-fluoro-22-methoxy-8,9,11,12,14,15-hexahydro-21H-4,6-ethenopyrimido[5,4-m][1,4,7,10,15]benzotetraoxazacycloheptadecine, Epidermal growth factor receptor | | 著者 | Beyett, T.S, Eck, M.J. | | 登録日 | 2022-03-10 | | 公開日 | 2022-11-23 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (3.42 Å) | | 主引用文献 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
J.Med.Chem., 65, 2022
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7U9A
 | | EGFR in complex with a macrocyclic inhibitor | | 分子名称: | 4-(5-chloro-4-fluoro-2-hydroxyanilino)-7-methoxyquinazolin-6-ol, CITRATE ANION, Epidermal growth factor receptor | | 著者 | Beyett, T.S, Eck, M.J. | | 登録日 | 2022-03-10 | | 公開日 | 2022-11-23 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
J.Med.Chem., 65, 2022
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8FV4
 | | EGFR(T790M/V948R) in complex with compound 2 (LN5993) | | 分子名称: | Epidermal growth factor receptor, MAGNESIUM ION, N-{(3P)-3-[(4P)-4-(2-acetamidopyridin-4-yl)-2-(methylsulfanyl)-1H-imidazol-5-yl]phenyl}-11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepine-9-carboxamide, ... | | 著者 | Ogboo, B.C, Beyett, T.S, Eck, M.J, Heppner, D.E. | | 登録日 | 2023-01-18 | | 公開日 | 2024-01-17 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors.
Commun Chem, 7, 2024
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6P1L
 | | Crystal structure of EGFR in complex with EAI045 | | 分子名称: | (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Heppner, D.E, Eck, M.J. | | 登録日 | 2019-05-20 | | 公開日 | 2019-12-18 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Acs Med.Chem.Lett., 10, 2019
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