5X2K
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5x2k by Molmil](/molmil-images/mine/5x2k) | Crystal structure of EGFR 696-1022 T790M in complex with WZ4003 | Descriptor: | Epidermal growth factor receptor, N-{3-[(5-chloro-2-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)oxy]phenyl}prop-2-enamide | Authors: | Zhu, S.J, Zhao, P, Yun, C.H. | Deposit date: | 2017-02-01 | Release date: | 2018-02-21 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (3.201 Å) | Cite: | Structural insights into drug development strategy targeting EGFR T790M/C797S. Oncotarget, 9, 2018
|
|
4TKS
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4tks by Molmil](/molmil-images/mine/4tks) | |
7K1I
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7k1i by Molmil](/molmil-images/mine/7k1i) | EGFR kinase (L858R/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: | 2020-09-07 | Release date: | 2021-09-15 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (3.202 Å) | Cite: | Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors Nat Commun, 13, 2022
|
|
6S9B
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 6s9b by Molmil](/molmil-images/mine/6s9b) | EGFR-KINASE IN COMPLEX WITH COMPOUND 1 | Descriptor: | 3-fluoranyl-~{N}-[1-(2-methyl-2-oxidanyl-propyl)benzimidazol-2-yl]-5-pyridin-3-yl-benzamide, Epidermal growth factor receptor | Authors: | Bader, G. | Deposit date: | 2019-07-12 | Release date: | 2019-11-20 | Last modified: | 2024-05-15 | Method: | X-RAY DIFFRACTION (3.25 Å) | Cite: | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. J.Med.Chem., 62, 2019
|
|
2ITO
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 2ito by Molmil](/molmil-images/mine/2ito) | Crystal structure of EGFR kinase domain G719S mutation in complex with Iressa | Descriptor: | EPIDERMAL GROWTH FACTOR RECEPTOR, Gefitinib | 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: | 2024-03-27 | Method: | X-RAY DIFFRACTION (3.25 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
|
|
5Y9T
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5y9t by Molmil](/molmil-images/mine/5y9t) | Crystal Structure of EGFR T790M mutant in complex with naquotinib | Descriptor: | 6-ethyl-3-[[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]amino]-5-[(3R)-1-prop-2-enoylpyrrolidin-3-yl]oxy-pyrazin e-2-carboxamide, Epidermal growth factor receptor | Authors: | Mimasu, S, Tomimoto, Y, Maiko, I, Yasushi, A, Tatsuya, N. | Deposit date: | 2017-08-28 | Release date: | 2018-07-11 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (3.25 Å) | Cite: | Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, inEGFR-Mutated Non-Small Cell Lung Cancer. Mol. Cancer Ther., 17, 2018
|
|
4R3R
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4r3r by Molmil](/molmil-images/mine/4r3r) | Crystal structures of EGFR in complex with Mig6 | Descriptor: | Epidermal growth factor receptor, peptide from ERBB receptor feedback inhibitor 1' | Authors: | 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. | Deposit date: | 2014-08-17 | Release date: | 2015-08-12 | Last modified: | 2015-09-16 | Method: | X-RAY DIFFRACTION (3.25 Å) | Cite: | Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6. Nat.Struct.Mol.Biol., 22, 2015
|
|
5JEB
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5jeb by Molmil](/molmil-images/mine/5jeb) | |
4WD5
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4wd5 by Molmil](/molmil-images/mine/4wd5) | Crystal structure of EGFR 696-1022 T790M in complex with QL-X138 | Descriptor: | CHLORIDE ION, Epidermal growth factor receptor, N-{2-methyl-5-[2-oxo-9-(1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-1(2H)-yl]phenyl}propanamide | Authors: | Yun, C.H, Eck, M.J. | Deposit date: | 2014-09-07 | Release date: | 2016-05-04 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3.3 Å) | Cite: | Crystal structure of EGFR 696-1022 T790M in complex with QL-X138 To Be Published
|
|
7SYE
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7sye by Molmil](/molmil-images/mine/7sye) | Cryo-EM structure of the extracellular module of the full-length EGFR bound to EGF. "tips-separated" 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 (3.3 Å) | Cite: | A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor. Elife, 10, 2021
|
|
7SZ0
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7sz0 by Molmil](/molmil-images/mine/7sz0) | Cryo-EM structure of the extracellular module of the full-length EGFR L834R 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: | 2021-11-25 | Release date: | 2021-12-22 | Method: | ELECTRON MICROSCOPY (3.3 Å) | Cite: | A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor. Elife, 10, 2021
|
|
3B2V
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 3b2v by Molmil](/molmil-images/mine/3b2v) | Crystal structure of the extracellular region of the epidermal growth factor receptor in complex with the Fab fragment of IMC-11F8 | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal growth factor receptor, ... | Authors: | Ferguson, K.M, Li, S, Kussie, P. | Deposit date: | 2007-10-19 | Release date: | 2008-02-19 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (3.3 Å) | Cite: | Structural basis for EGF receptor inhibition by the therapeutic antibody IMC-11F8. Structure, 16, 2008
|
|
1IVO
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 1ivo by Molmil](/molmil-images/mine/1ivo) | Crystal Structure of the Complex of Human Epidermal Growth Factor and Receptor Extracellular Domains. | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal Growth Factor Receptor, ... | Authors: | Ogiso, H, Ishitani, R, Nureki, O, Fukai, S, Yamanaka, M, Kim, J.H, Saito, K, Shirouzu, M, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI) | Deposit date: | 2002-03-28 | Release date: | 2002-10-16 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (3.3 Å) | Cite: | Crystal Structure of the Complex of Human Epidermal Growth Factor and Receptor Extracellular Domains. Cell(Cambridge,Mass.), 110, 2002
|
|
8UKX
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8ukx by Molmil](/molmil-images/mine/8ukx) | |
3NJP
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 3njp by Molmil](/molmil-images/mine/3njp) | The Extracellular and Transmembrane Domain Interfaces in Epidermal Growth Factor Receptor Signaling | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal growth factor, Epidermal growth factor receptor, ... | Authors: | Lu, C, Mi, L.-Z, Grey, M.J, Zhu, J, Graef, E, Yokoyama, S, Springer, T.A. | Deposit date: | 2010-06-17 | Release date: | 2010-10-13 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (3.304 Å) | Cite: | Structural evidence for loose linkage between ligand binding and kinase activation in the epidermal growth factor receptor. Mol.Cell.Biol., 30, 2010
|
|
8HGO
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8hgo by Molmil](/molmil-images/mine/8hgo) | The EGF-bound EGFR/HER2 ectodomain complex | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal growth factor, ... | Authors: | Zhang, Z, Bai, X. | Deposit date: | 2022-11-15 | Release date: | 2023-02-08 | Last modified: | 2023-03-01 | Method: | ELECTRON MICROSCOPY (3.31 Å) | Cite: | Structure and dynamics of the EGFR/HER2 heterodimer. Cell Discov, 9, 2023
|
|
8EME
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8eme by Molmil](/molmil-images/mine/8eme) | EGFR(T790M/V948R) in complex with ZNL-0056 | Descriptor: | Epidermal growth factor receptor, N-{7-methyl-1-[(3S)-1-(prop-2-enoyl)azepan-3-yl]-1H-benzimidazol-2-yl}-5-(prop-2-enamido)thiophene-3-carboxamide | Authors: | Beyett, T.S, Eck, M.J. | Deposit date: | 2022-09-27 | Release date: | 2023-10-18 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (3.32 Å) | Cite: | Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality Acs Cent.Sci., 2024
|
|
4I20
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4i20 by Molmil](/molmil-images/mine/4i20) | Crystal structure of monomeric (V948R) primary oncogenic mutant L858R EGFR kinase domain | Descriptor: | Epidermal growth factor receptor | Authors: | Gajiwala, K.S, Feng, J, Ferre, R, Ryan, K, Brodsky, O, Stewart, A. | Deposit date: | 2012-11-21 | Release date: | 2013-01-16 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (3.34 Å) | Cite: | Insights into the Aberrant Activity of Mutant EGFR Kinase Domain and Drug Recognition. Structure, 21, 2013
|
|
4I21
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 4i21 by Molmil](/molmil-images/mine/4i21) | Crystal structure of L858R + T790M EGFR kinase domain in complex with MIG6 peptide | Descriptor: | ERBB receptor feedback inhibitor 1, Epidermal growth factor receptor | Authors: | Gajiwala, K.S, Feng, J, Ferre, R, Ryan, K, Brodsky, O, Stewart, A. | Deposit date: | 2012-11-21 | Release date: | 2013-01-16 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (3.37 Å) | Cite: | Insights into the Aberrant Activity of Mutant EGFR Kinase Domain and Drug Recognition. Structure, 21, 2013
|
|
7SZ7
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7sz7 by Molmil](/molmil-images/mine/7sz7) | Cryo-EM structure of the extracellular module of the full-length EGFR bound to TGF-alpha. "tips-juxtaposed" conformation | Descriptor: | Epidermal growth factor receptor, Transforming growth factor alpha | Authors: | Huang, Y, Ognjenovic, J, Karandur, D, Miller, K, Merk, A, Subramaniam, S, Kuriyan, J. | Deposit date: | 2021-11-25 | Release date: | 2021-12-15 | Method: | ELECTRON MICROSCOPY (3.4 Å) | Cite: | A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor. Elife, 10, 2021
|
|
7SZ1
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7sz1 by Molmil](/molmil-images/mine/7sz1) | Cryo-EM structure of the extracellular module of the full-length EGFR L834R bound to EGF. "tips-separated" 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: | 2021-11-25 | Release date: | 2021-12-22 | Method: | ELECTRON MICROSCOPY (3.4 Å) | Cite: | A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor. Elife, 10, 2021
|
|
5FEQ
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 5feq by Molmil](/molmil-images/mine/5feq) | EGFR KINASE DOMAIN IN COMPLEX WITH A COVALENT AMINOBENZIMIDAZOLE | Descriptor: | Epidermal growth factor receptor, ~{N}-[1-[(3~{R})-1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl]-7-methyl-benzimidazol-2-yl]-2-methyl-pyridine-4-carboxamide | Authors: | DiDonato, M, Spraggon, G. | Deposit date: | 2015-12-17 | Release date: | 2016-07-27 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (3.4 Å) | Cite: | Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers. J.Med.Chem., 59, 2016
|
|
8H7X
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 8h7x by Molmil](/molmil-images/mine/8h7x) | Crystal structure of EGFR T790M/C797S mutant in complex with brigatinib | Descriptor: | 5-chloro-N~4~-[2-(dimethylphosphoryl)phenyl]-N~2~-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine, Epidermal growth factor receptor | Authors: | Kukimoto-Niino, M, Shirouzu, M. | Deposit date: | 2022-10-21 | Release date: | 2023-10-25 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (3.404 Å) | Cite: | A macrocyclic kinase inhibitor overcomes triple resistant mutations in EGFR-positive lung cancer. NPJ Precis Oncol, 8, 2024
|
|
7U98
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 7u98 by Molmil](/molmil-images/mine/7u98) | EGFR(T790M/V948R) in complex with a macrocyclic inhibitor | Descriptor: | 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 | Authors: | Beyett, T.S, Eck, M.J. | Deposit date: | 2022-03-10 | Release date: | 2022-11-23 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (3.42 Å) | Cite: | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. J.Med.Chem., 65, 2022
|
|
2ITY
![Download](/newweb/media/icons/dl.png) ![Visualize](/newweb/media/icons/hoh_3d.png)
![BU of 2ity by Molmil](/molmil-images/mine/2ity) | Crystal structure of EGFR kinase domain in complex with Iressa | Descriptor: | EPIDERMAL GROWTH FACTOR RECEPTOR, Gefitinib | 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: | 2024-03-27 | Method: | X-RAY DIFFRACTION (3.42 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
|
|