5XGN
 
 | | Crystal structure of EGFR 696-1022 T790M/C797S in complex with Go6976 | | Descriptor: | 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole, CHLORIDE ION, Epidermal growth factor receptor | | Authors: | Kong, L.L, Yun, C.H. | | Deposit date: | 2017-04-14 | | Release date: | 2017-10-11 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structural pharmacological studies on EGFR T790M/C797S.
Biochem. Biophys. Res. Commun., 488, 2017
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7JXI
 | | EGFR kinase (T790M/V948R) in complex with PF-06747775 | | Descriptor: | Epidermal growth factor receptor, N-[(3R,4R)-4-fluoro-1-{6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl}pyrrolidin-3-yl]propanamide | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2020-08-27 | | Release date: | 2021-09-08 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors
Nat Commun, 13, 2022
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5WB8
 | | Crystal structure of the epidermal growth factor receptor extracellular region in complex with epigen | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal growth factor receptor, Epigen, ... | | Authors: | Bessman, N.J, Freed, D.M, Moore, J.O, Ferguson, K.M, Lemmon, M.A. | | Deposit date: | 2017-06-28 | | Release date: | 2017-10-18 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | EGFR Ligands Differentially Stabilize Receptor Dimers to Specify Signaling Kinetics.
Cell, 171, 2017
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5C8K
 | | EGFR kinase domain mutant "TMLR" with compound 1 | | Descriptor: | 1-cyclopentyl-N-[2-(4-methoxypiperidin-1-yl)pyrimidin-4-yl]-1H-imidazo[4,5-c]pyridin-6-amine, Epidermal growth factor receptor | | Authors: | Eigenbrot, C, Yu, C. | | Deposit date: | 2015-06-25 | | Release date: | 2015-10-28 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.
J.Med.Chem., 58, 2015
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4R5S
 | | Crystal structure of EGFR 696-1022 L858R in complex with FIIN-3 | | Descriptor: | Epidermal growth factor receptor, N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide | | Authors: | Zhu, S.J, Yun, C.H. | | Deposit date: | 2014-08-22 | | Release date: | 2014-11-12 | | Last modified: | 2022-08-24 | | Method: | X-RAY DIFFRACTION (3.001 Å) | | Cite: | Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Proc.Natl.Acad.Sci.USA, 111, 2014
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2JIU
 | | Crystal structure of EGFR kinase domain T790M mutation in complex with AEE788 | | Descriptor: | 6-{4-[(4-ETHYLPIPERAZIN-1-YL)METHYL]PHENYL}-N-[(1R)-1-PHENYLETHYL]-7H-PYRROLO[2,3-D]PYRIMIDIN-4-AMINE, EPIDERMAL GROWTH FACTOR RECEPTOR | | Authors: | Yun, C.-H, Mengwasser, K.E, Toms, A.V, Woo, M.S, Greulich, H, Wong, K.-K, Meyerson, M, Eck, M.J. | | Deposit date: | 2007-07-01 | | Release date: | 2008-01-22 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (3.05 Å) | | Cite: | The T790M Mutation in Egfr Kinase Causes Drug Resistance by Increasing the Affinity for ATP.
Proc.Natl.Acad.Sci.USA, 105, 2008
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4KRO
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5UWD
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7SYD
 | | Cryo-EM structure of the extracellular module of the full-length EGFR bound to EGF "tips-juxtaposed" conformation | | Descriptor: | Epidermal growth factor, Epidermal growth factor receptor | | Authors: | Huang, Y, Ognjenovic, J, Karandur, D, Miller, K, Merk, A, Subramaniam, S, Kuriyan, J. | | Deposit date: | 2021-11-24 | | Release date: | 2021-12-22 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor.
Elife, 10, 2021
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7KY0
 | | Inactive conformation of EGFR (T790M/V948R) kinase in complex with BI-4020 | | Descriptor: | (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 | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2020-12-06 | | Release date: | 2022-01-19 | | Last modified: | 2024-05-29 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Structural Analysis of the Macrocyclic Inhibitor BI-4020 Binding to EGFR Kinase.
Chemmedchem, 2024
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4RJ5
 | | EGFR kinase (T790M/L858R) with inhibitor compound 5 | | Descriptor: | Epidermal growth factor receptor, N-[2-(4-methoxypiperidin-1-yl)pyrimidin-4-yl]-2-(1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]pyridin-6-amine | | Authors: | Eigenbrot, C, Yu, C. | | Deposit date: | 2014-10-08 | | Release date: | 2014-11-26 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation.
J.Med.Chem., 57, 2014
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4RIW
 | | Crystal structure of an EGFR/HER3 kinase domain heterodimer | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, Epidermal growth factor receptor, MAGNESIUM ION, ... | | Authors: | Littlefield, P, Jura, N. | | Deposit date: | 2014-10-07 | | Release date: | 2014-12-10 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Structural analysis of the EGFR/HER3 heterodimer reveals the molecular basis for activating HER3 mutations.
Sci.Signal., 7, 2014
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4RIX
 | | Crystal structure of an EGFR/HER3 kinase domain heterodimer containing the cancer-associated HER3-Q790R mutation | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, Epidermal growth factor receptor, MAGNESIUM ION, ... | | Authors: | Littlefield, P, Liu, L, Jura, N. | | Deposit date: | 2014-10-07 | | Release date: | 2014-12-10 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Structural analysis of the EGFR/HER3 heterodimer reveals the molecular basis for activating HER3 mutations.
Sci.Signal., 7, 2014
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2JIT
 | | Crystal structure of EGFR kinase domain T790M mutation | | Descriptor: | EPIDERMAL GROWTH FACTOR RECEPTOR | | Authors: | Yun, C.-H, Mengwasser, K.E, Toms, A.V, Woo, M.S, Greulich, H, Wong, K.-K, Meyerson, M, Eck, M.J. | | Deposit date: | 2007-07-01 | | Release date: | 2008-01-22 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | The T790M Mutation in Egfr Kinase Causes Drug Resistance by Increasing the Affinity for ATP.
Proc.Natl.Acad.Sci.USA, 105, 2008
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2J6M
 | | Crystal structure of EGFR kinase domain in complex with AEE788 | | Descriptor: | 6-{4-[(4-ETHYLPIPERAZIN-1-YL)METHYL]PHENYL}-N-[(1R)-1-PHENYLETHYL]-7H-PYRROLO[2,3-D]PYRIMIDIN-4-AMINE, EPIDERMAL GROWTH FACTOR RECEPTOR | | Authors: | Yun, C.-H, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | Deposit date: | 2006-09-29 | | Release date: | 2007-04-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | 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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7LGS
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2J5E
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7JXK
 | | EGFR kinase (T790M/V948R) in complex with PF-06747775 and JBJ-04-125-02 | | Descriptor: | (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-{1-oxo-6-[4-(piperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindol-2-yl}-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, MAGNESIUM ION, ... | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2020-08-27 | | Release date: | 2021-09-08 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors
Nat Commun, 13, 2022
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5Y25
 | | EGFR kinase domain mutant (T790M/L858R) with covalent ligand NS-062 | | Descriptor: | (2R)-N-[4-[(3-chloranyl-4-fluoranyl-phenyl)amino]-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]-1-(2-fluoranylethanoyl)pyrrolidine-2-carboxamide, Epidermal growth factor receptor | | Authors: | Shiroishi, M, Abe, Y, Caaveiro, J.M.M, Sakamoto, S, Morimoto, S, Fuchida, H, Shindo, N, Ojida, A. | | Deposit date: | 2017-07-24 | | Release date: | 2018-07-25 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (3.102 Å) | | Cite: | Selective and reversible modification of kinase cysteines with chlorofluoroacetamides.
Nat.Chem.Biol., 15, 2019
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5GTY
 | | Crystal structure of EGFR 696-1022 T790M in complex with LXX-6-26 | | Descriptor: | 1,2-ETHANEDIOL, 1-[(3R)-3-[4-azanyl-3-[3-chloranyl-4-[(6-methylpyridin-2-yl)methoxy]phenyl]pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one, Epidermal growth factor receptor | | Authors: | Yan, X.E, Yun, C.H. | | Deposit date: | 2016-08-23 | | Release date: | 2017-09-06 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (3.14 Å) | | Cite: | Discovery and characterization of a novel irreversible EGFR mutants selective and potent kinase inhibitor CHMFL-EGFR-26 with a distinct binding mode.
Oncotarget, 8, 2017
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4G5P
 | | Crystal structure of EGFR kinase T790M in complex with BIBW2992 | | Descriptor: | Epidermal growth factor receptor, N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[(3S)-tetrahydrofuran-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)butanamide | | Authors: | Solca, F, Dahl, G, Zoephel, A, Bader, G, Sanderson, M, Klein, C, Kraemer, O, Himmelsbach, F, Haaksma, E, Adolf, G.R. | | Deposit date: | 2012-07-18 | | Release date: | 2012-08-29 | | Last modified: | 2012-10-31 | | Method: | X-RAY DIFFRACTION (3.17 Å) | | Cite: | Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker.
J.Pharmacol.Exp.Ther., 343, 2012
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3C09
 | | Crystal structure the Fab fragment of matuzumab (Fab72000) in complex with domain III of the extracellular region of EGFR | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal growth factor receptor, Matuzumab Fab Heavy chain, ... | | Authors: | Ferguson, K.M, Schmiedel, J, Knoechel, T. | | Deposit date: | 2008-01-18 | | Release date: | 2008-04-15 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization.
Cancer Cell, 13, 2008
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7LFR
 | | Crystal structure of the epidermal growth factor receptor extracellular region with R84K mutation in complex with epiregulin crystallized with spermine | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal growth factor receptor, Proepiregulin, ... | | Authors: | Hu, C, Leche II, C.A, Stayrook, S.E, Ferguson, K.M, Lemmon, M.A. | | Deposit date: | 2021-01-18 | | Release date: | 2021-11-17 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Glioblastoma mutations alter EGFR dimer structure to prevent ligand bias.
Nature, 602, 2022
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8F1W
 | | EGFR(T790M/V948R) kinase in complex with poziotinib | | Descriptor: | 1-[4-[4-[[3,4-bis(chloranyl)-2-fluoranyl-phenyl]amino]-7-methoxy-quinazolin-6-yl]oxypiperidin-1-yl]propan-1-one, Epidermal growth factor receptor | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2022-11-06 | | Release date: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | EGFR(T790M/V948R) kinase in complex with poziotinib
To be published
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6ARU
 | | Structure of Cetuximab Fab mutant in complex with EGFR extracellular domain | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Cetuximab mutant heavy chain Fab fragment,Immunoglobulin gamma-1 heavy chain, ... | | Authors: | Christie, M, Christ, D. | | Deposit date: | 2017-08-23 | | Release date: | 2018-08-29 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Structure of Cetuximab Fab mutant in complex with EGFR extracellular domain
To Be Published
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