6V5P
 
 | | EGFR(T790M/V948R) in complex with LN2725 | | Descriptor: | 4-[4-(4-fluorophenyl)-2-(3-methoxypropyl)-1H-imidazol-5-yl]-2-phenyl-3H-pyrrolo[2,3-b]pyridine, CHLORIDE ION, Epidermal growth factor receptor | | Authors: | Heppner, D.E, Eck, M.J. | | Deposit date: | 2019-12-04 | | Release date: | 2020-04-22 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | 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 | | Descriptor: | Epidermal growth factor receptor, N-[3-({4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl}amino)-4-methoxyphenyl]propanamide | | Authors: | Heppner, D.E, Eck, M.J. | | Deposit date: | 2020-01-10 | | Release date: | 2020-04-22 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.
J.Med.Chem., 63, 2020
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1NHL
 | | SNAP-23N Structure | | Descriptor: | Synaptosomal-associated protein 23 | | Authors: | Freedman, S.J, Song, H.K, Xu, Y, Eck, M.J. | | Deposit date: | 2002-12-19 | | Release date: | 2003-04-15 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Homotetrameric Structure of the SNAP-23 N-terminal Coiled-coil Domain
J.Biol.Chem., 278, 2003
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6WA2
 | | Crystal structure of EGFR(T790M/V948R) in complex with LN3753 | | Descriptor: | CHLORIDE ION, Epidermal growth factor receptor, N-(3-{5-[2-(acetylamino)pyridin-4-yl]-2-(methylsulfanyl)-1H-imidazol-4-yl}phenyl)-2-fluoro-5-hydroxybenzamide | | Authors: | Heppner, D.E, Eck, M.J. | | Deposit date: | 2020-03-24 | | Release date: | 2021-03-31 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | 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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6WAK
 | | A crystal structure of EGFR(T790M/V948R) in complex with LN3754 | | Descriptor: | Epidermal growth factor receptor, MAGNESIUM ION, N-(3-{5-[2-(acetylamino)pyridin-4-yl]-2-(methylsulfanyl)-1H-imidazol-4-yl}phenyl)-2-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]benzamide, ... | | Authors: | Heppner, D.E, Eck, M.J. | | Deposit date: | 2020-03-25 | | Release date: | 2021-03-31 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | 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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1NTV
 | | Crystal Structure of the Disabled-1 (Dab1) PTB domain-ApoER2 peptide complex | | Descriptor: | Apolipoprotein E Receptor-2 peptide, Disabled homolog 1, PHOSPHATE ION | | Authors: | Stolt, P.C, Jeon, H, Song, H.K, Herz, J, Eck, M.J, Blacklow, S.C. | | Deposit date: | 2003-01-30 | | Release date: | 2003-04-15 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Origins of Peptide Selectivity and Phosphoinositide Binding Revealed by Structures of Disabled-1 PTB Domain Complexes
Structure, 11, 2003
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1Q69
 | | Solution structure of T-cell surface glycoprotein CD8 alpha chain and Proto-oncogene tyrosine-protein kinase LCK fragments | | Descriptor: | Proto-oncogene tyrosine-protein kinase LCK, T-cell surface glycoprotein CD8 alpha chain, ZINC ION | | Authors: | Kim, P.W, Sun, Z.Y, Blacklow, S.C, Wagner, G, Eck, M.J. | | Deposit date: | 2003-08-12 | | Release date: | 2003-11-25 | | Last modified: | 2024-05-22 | | Method: | SOLUTION NMR | | Cite: | A zinc clasp structure tethers Lck to T cell coreceptors CD4 and CD8.
Science, 301, 2003
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6WXN
 | | EGFR(T790M/V948R) in complex with LN3844 | | Descriptor: | CHLORIDE ION, Epidermal growth factor receptor, MAGNESIUM ION, ... | | Authors: | Heppner, D.E, Eck, M.J. | | Deposit date: | 2020-05-11 | | Release date: | 2021-05-19 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.76 Å) | | Cite: | 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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1OX9
 | | Crystal structure of SspB-ssrA complex | | Descriptor: | Stringent starvation protein B, ssrA | | Authors: | Song, H.K, Eck, M.J. | | Deposit date: | 2003-04-01 | | Release date: | 2003-08-26 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structural basis of degradation signal recognition by SspB, a specificity-enhancing factor for the ClpXP proteolytic machine
Mol.Cell, 12, 2003
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1Q68
 | | Solution structure of T-cell surface glycoprotein CD4 and Proto-oncogene tyrosine-protein kinase LCK fragments | | Descriptor: | Proto-oncogene tyrosine-protein kinase LCK, T-cell surface glycoprotein CD4, ZINC ION | | Authors: | Kim, P.W, Sun, Z.Y, Blacklow, S.C, Wagner, G, Eck, M.J. | | Deposit date: | 2003-08-12 | | Release date: | 2003-11-25 | | Last modified: | 2024-05-22 | | Method: | SOLUTION NMR | | Cite: | A zinc clasp structure tethers Lck to T cell coreceptors CD4 and CD8.
Science, 301, 2003
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1NU2
 | | Crystal structure of the murine Disabled-1 (Dab1) PTB domain-ApoER2 peptide-PI-4,5P2 ternary complex | | Descriptor: | D-MYO-INOSITOL-1,4,5-TRIPHOSPHATE, Disabled homolog 1, peptide derived from murine Apolipoprotein E Receptor-2 | | Authors: | Stolt, P.C, Jeon, H, Song, H.K, Herz, J, Eck, M.J, Blacklow, S.C. | | Deposit date: | 2003-01-30 | | Release date: | 2003-04-15 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Origins of Peptide Selectivity and Phosphoinositide Binding Revealed by Structures of Disabled-1 PTB Domain Complexes
Structure, 11, 2003
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3ZDT
 | | Crystal structure of basic patch mutant FAK FERM domain FAK31- 405 K216A, K218A, R221A, K222A | | Descriptor: | FOCAL ADHESION KINASE 1 | | Authors: | Goni, G.M, Epifano, C, Boskovic, J, Camacho-Artacho, M, Zhou, J, Martin, M.T, Eck, M.J, Kremer, L, Graeter, F, Gervasio, F.L, Perez-Moreno, M, Lietha, D. | | Deposit date: | 2012-11-30 | | Release date: | 2012-12-12 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (3.15 Å) | | Cite: | Phosphatidylinositol 4,5-Bisphosphate Triggers Activation of Focal Adhesion Kinase by Inducing Clustering and Conformational Changes.
Proc.Natl.Acad.Sci.USA, 111, 2014
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7JXH
 | | HER2 in complex with JBJ-08-178-01 | | Descriptor: | (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 | | 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 (3.27 Å) | | Cite: | 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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7JXQ
 | | EGFR kinase (T790M/V948R) in complex with allosteric inhibitor JBJ-09-063 | | Descriptor: | (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, ... | | 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 (1.83 Å) | | Cite: | 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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2ITT
 | | Crystal structure of EGFR kinase domain L858R 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, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | Deposit date: | 2006-05-25 | | Release date: | 2007-04-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.73 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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2J0M
 | | Crystal structure a two-chain complex between the FERM and kinase domains of focal adhesion kinase. | | Descriptor: | 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Cai, X, Li, Y, Schaller, M.D, Eck, M.J. | | Deposit date: | 2006-08-03 | | Release date: | 2007-07-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structural Basis for the Autoinhibition of Focal Adhesion Kinase.
Cell(Cambridge,Mass.), 129, 2007
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2J0K
 | | Crystal structure of a fragment of focal adhesion kinase containing the FERM and kinase domains. | | Descriptor: | 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Cai, X, Li, Y, Schaller, M.D, Eck, M.J. | | Deposit date: | 2006-08-03 | | Release date: | 2007-07-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structural Basis for the Autoinhibition of Focal Adhesion Kinase.
Cell(Cambridge,Mass.), 129, 2007
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2ITN
 | | Crystal structure of EGFR kinase domain G719S mutation in complex with AMP-PNP | | Descriptor: | EPIDERMAL GROWTH FACTOR RECEPTOR, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | Authors: | Yun, C.-H, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | Deposit date: | 2006-05-25 | | Release date: | 2007-04-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.47 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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2J0J
 | | Crystal structure of a fragment of focal adhesion kinase containing the FERM and kinase domains. | | Descriptor: | 1,2,3,4-TETRAHYDROGEN-STAUROSPORINE, FOCAL ADHESION KINASE 1 | | Authors: | Lietha, D, Cai, X, Li, Y, Schaller, M.D, Eck, M.J. | | Deposit date: | 2006-08-03 | | Release date: | 2007-06-26 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structural Basis for the Autoinhibition of Focal Adhesion Kinase
Cell(Cambridge,Mass.), 129, 2007
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2J0L
 | | Crystal structure of a the active conformation of the kinase domain of focal adhesion kinase with a phosphorylated activation loop. | | Descriptor: | FOCAL ADHESION KINASE 1, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Lietha, D, Cai, X, Li, Y, Schaller, M.D, Eck, M.J. | | Deposit date: | 2006-08-03 | | Release date: | 2007-06-26 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural Basis for the Autoinhibition of Focal Adhesion Kinase
Cell(Cambridge,Mass.), 129, 2007
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2ITQ
 | | Crystal structure of EGFR kinase domain G719S mutation in complex with AFN941 | | Descriptor: | 1,2,3,4-Tetrahydrogen Staurosporine, EPIDERMAL GROWTH FACTOR RECEPTOR | | Authors: | Yun, C.-H, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | Deposit date: | 2006-05-25 | | Release date: | 2007-04-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.68 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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2ITV
 | | Crystal structure of EGFR kinase domain L858R mutation in complex with AMP-PNP | | Descriptor: | EPIDERMAL GROWTH FACTOR RECEPTOR, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | Authors: | Yun, C.-H, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | Deposit date: | 2006-05-25 | | Release date: | 2007-04-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.47 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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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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2J5F
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7JXP
 | | EGFR kinase (T790M/V948R) in complex with osimertinib 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 (2.16 Å) | | Cite: | Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors
Nat Commun, 13, 2022
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