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PDB: 317 件
5X2K
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BU of 5x2k by Molmil
Crystal structure of EGFR 696-1022 T790M in complex with WZ4003
分子名称: 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
著者Zhu, S.J, Zhao, P, Yun, C.H.
登録日2017-02-01
公開日2018-02-21
最終更新日2024-03-27
実験手法X-RAY DIFFRACTION (3.201 Å)
主引用文献Structural insights into drug development strategy targeting EGFR T790M/C797S.
Oncotarget, 9, 2018
4TKS
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BU of 4tks by Molmil
Native-SAD phasing for human EGFR kinase domain.
分子名称: Epidermal growth factor receptor
著者Cai, Z, Greene, M.I, Liu, Q.
登録日2014-05-27
公開日2014-10-08
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (3.2017 Å)
主引用文献Multi-crystal native SAD analysis at 6 keV.
Acta Crystallogr.,Sect.D, 70, 2014
7K1I
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BU of 7k1i by Molmil
EGFR kinase (L858R/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2020-09-07
公開日2021-09-15
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (3.202 Å)
主引用文献Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors
Nat Commun, 13, 2022
2ITO
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BU of 2ito by Molmil
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
6S9B
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BU of 6s9b by Molmil
EGFR-KINASE IN COMPLEX WITH COMPOUND 1
分子名称: 3-fluoranyl-~{N}-[1-(2-methyl-2-oxidanyl-propyl)benzimidazol-2-yl]-5-pyridin-3-yl-benzamide, Epidermal growth factor receptor
著者Bader, G.
登録日2019-07-12
公開日2019-11-20
最終更新日2024-05-15
実験手法X-RAY DIFFRACTION (3.25 Å)
主引用文献Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.
J.Med.Chem., 62, 2019
5Y9T
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BU of 5y9t by Molmil
Crystal Structure of EGFR T790M mutant in complex with naquotinib
分子名称: 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
著者Mimasu, S, Tomimoto, Y, Maiko, I, Yasushi, A, Tatsuya, N.
登録日2017-08-28
公開日2018-07-11
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (3.25 Å)
主引用文献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
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BU of 4r3r by Molmil
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 (3.25 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
5JEB
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BU of 5jeb by Molmil
Crystal structure of EGFR tyrosine kinase domain with novel inhibitor of active state of HER2
分子名称: 3-(furan-2-yl)-N-[5-(furan-2-yl)-2-methoxyphenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Epidermal growth factor receptor, SULFATE ION
著者Park, J.H, Lemmon, M.A.
登録日2016-04-18
公開日2016-09-07
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (3.298 Å)
主引用文献Overcoming resistance to HER2 inhibitors through state-specific kinase binding.
Nat.Chem.Biol., 12, 2016
4WD5
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BU of 4wd5 by Molmil
Crystal structure of EGFR 696-1022 T790M in complex with QL-X138
分子名称: 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
著者Yun, C.H, Eck, M.J.
登録日2014-09-07
公開日2016-05-04
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (3.3 Å)
主引用文献Crystal structure of EGFR 696-1022 T790M in complex with QL-X138
To Be Published
7SYE
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BU of 7sye by Molmil
Cryo-EM structure of the extracellular module of the full-length EGFR bound to EGF. "tips-separated" conformation
分子名称: Epidermal growth factor, Epidermal growth factor receptor
著者Huang, Y, Ognjenovic, J, Karandur, D, Miller, K, Merk, A, Subramaniam, S, Kuriyan, J.
登録日2021-11-24
公開日2021-12-22
実験手法ELECTRON MICROSCOPY (3.3 Å)
主引用文献A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor.
Elife, 10, 2021
7SZ0
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BU of 7sz0 by Molmil
Cryo-EM structure of the extracellular module of the full-length EGFR L834R bound to EGF. "tips-juxtaposed" conformation
分子名称: Epidermal growth factor, Epidermal growth factor receptor
著者Huang, Y, Ognjenovic, J, Karandur, D, Miller, K, Merk, A, Subramaniam, S, Kuriyan, J.
登録日2021-11-25
公開日2021-12-22
実験手法ELECTRON MICROSCOPY (3.3 Å)
主引用文献A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor.
Elife, 10, 2021
3B2V
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BU of 3b2v by Molmil
Crystal structure of the extracellular region of the epidermal growth factor receptor in complex with the Fab fragment of IMC-11F8
分子名称: 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, ...
著者Ferguson, K.M, Li, S, Kussie, P.
登録日2007-10-19
公開日2008-02-19
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (3.3 Å)
主引用文献Structural basis for EGF receptor inhibition by the therapeutic antibody IMC-11F8.
Structure, 16, 2008
1IVO
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BU of 1ivo by Molmil
Crystal Structure of the Complex of Human Epidermal Growth Factor and Receptor Extracellular Domains.
分子名称: 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, ...
著者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)
登録日2002-03-28
公開日2002-10-16
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (3.3 Å)
主引用文献Crystal Structure of the Complex of Human Epidermal Growth Factor and Receptor Extracellular Domains.
Cell(Cambridge,Mass.), 110, 2002
8UKX
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BU of 8ukx by Molmil
Crystal structure the extracellular region of the epidermal growth factor receptor variant III (EGFRvIII) at pH 7.0
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal growth factor receptor, alpha-L-fucopyranose-(1-6)-2-acetamido-2-deoxy-beta-D-glucopyranose
著者Stayrook, S.E, Ferguson, K.M.
登録日2023-10-15
公開日2024-06-12
最終更新日2024-07-03
実験手法X-RAY DIFFRACTION (3.301 Å)
主引用文献Structural insights into the role and targeting of EGFRvIII.
Structure, 2024
3NJP
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BU of 3njp by Molmil
The Extracellular and Transmembrane Domain Interfaces in Epidermal Growth Factor Receptor Signaling
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, Epidermal growth factor, Epidermal growth factor receptor, ...
著者Lu, C, Mi, L.-Z, Grey, M.J, Zhu, J, Graef, E, Yokoyama, S, Springer, T.A.
登録日2010-06-17
公開日2010-10-13
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (3.304 Å)
主引用文献Structural evidence for loose linkage between ligand binding and kinase activation in the epidermal growth factor receptor.
Mol.Cell.Biol., 30, 2010
8HGO
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BU of 8hgo by Molmil
The EGF-bound EGFR/HER2 ectodomain complex
分子名称: 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, ...
著者Zhang, Z, Bai, X.
登録日2022-11-15
公開日2023-02-08
最終更新日2023-03-01
実験手法ELECTRON MICROSCOPY (3.31 Å)
主引用文献Structure and dynamics of the EGFR/HER2 heterodimer.
Cell Discov, 9, 2023
8EME
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BU of 8eme by Molmil
EGFR(T790M/V948R) in complex with ZNL-0056
分子名称: 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
著者Beyett, T.S, Eck, M.J.
登録日2022-09-27
公開日2023-10-18
最終更新日2024-07-10
実験手法X-RAY DIFFRACTION (3.32 Å)
主引用文献Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality.
Acs Cent.Sci., 10, 2024
4I20
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BU of 4i20 by Molmil
Crystal structure of monomeric (V948R) primary oncogenic mutant L858R EGFR kinase domain
分子名称: Epidermal growth factor receptor
著者Gajiwala, K.S, Feng, J, Ferre, R, Ryan, K, Brodsky, O, Stewart, A.
登録日2012-11-21
公開日2013-01-16
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (3.34 Å)
主引用文献Insights into the Aberrant Activity of Mutant EGFR Kinase Domain and Drug Recognition.
Structure, 21, 2013
4I21
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BU of 4i21 by Molmil
Crystal structure of L858R + T790M EGFR kinase domain in complex with MIG6 peptide
分子名称: ERBB receptor feedback inhibitor 1, Epidermal growth factor receptor
著者Gajiwala, K.S, Feng, J, Ferre, R, Ryan, K, Brodsky, O, Stewart, A.
登録日2012-11-21
公開日2013-01-16
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (3.37 Å)
主引用文献Insights into the Aberrant Activity of Mutant EGFR Kinase Domain and Drug Recognition.
Structure, 21, 2013
7SZ7
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BU of 7sz7 by Molmil
Cryo-EM structure of the extracellular module of the full-length EGFR bound to TGF-alpha. "tips-juxtaposed" conformation
分子名称: Epidermal growth factor receptor, Transforming growth factor alpha
著者Huang, Y, Ognjenovic, J, Karandur, D, Miller, K, Merk, A, Subramaniam, S, Kuriyan, J.
登録日2021-11-25
公開日2021-12-15
実験手法ELECTRON MICROSCOPY (3.4 Å)
主引用文献A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor.
Elife, 10, 2021
7SZ1
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BU of 7sz1 by Molmil
Cryo-EM structure of the extracellular module of the full-length EGFR L834R bound to EGF. "tips-separated" conformation
分子名称: Epidermal growth factor, Epidermal growth factor receptor
著者Huang, Y, Ognjenovic, J, Karandur, D, Miller, K, Merk, A, Subramaniam, S, Kuriyan, J.
登録日2021-11-25
公開日2021-12-22
実験手法ELECTRON MICROSCOPY (3.4 Å)
主引用文献A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor.
Elife, 10, 2021
5FEQ
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BU of 5feq by Molmil
EGFR KINASE DOMAIN IN COMPLEX WITH A COVALENT AMINOBENZIMIDAZOLE
分子名称: 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
著者DiDonato, M, Spraggon, G.
登録日2015-12-17
公開日2016-07-27
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (3.4 Å)
主引用文献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
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BU of 8h7x by Molmil
Crystal structure of EGFR T790M/C797S mutant in complex with brigatinib
分子名称: 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
著者Kukimoto-Niino, M, Shirouzu, M.
登録日2022-10-21
公開日2023-10-25
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (3.404 Å)
主引用文献A macrocyclic kinase inhibitor overcomes triple resistant mutations in EGFR-positive lung cancer.
NPJ Precis Oncol, 8, 2024
7U98
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BU of 7u98 by Molmil
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
2ITY
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BU of 2ity by Molmil
Crystal structure of EGFR kinase domain 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 (3.42 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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