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
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5D41
 | | EGFR kinase domain in complex with mutant selective allosteric inhibitor | | Descriptor: | (2R)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-2-phenyl-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, MAGNESIUM ION, ... | | Authors: | Yun, C.-H, Park, E, Eck, M.J. | | Deposit date: | 2015-08-07 | | Release date: | 2016-06-08 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.31 Å) | | Cite: | Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.
Nature, 534, 2016
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5CZH
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5CZI
 | | EGFR L858R MUTANT IN COMPLEX WITH A SHC PEPTIDE SUBSTRATE | | Descriptor: | Epidermal growth factor receptor, SHC Peptide substrate | | Authors: | Yun, C.H, Eck, M.J. | | Deposit date: | 2015-07-31 | | Release date: | 2015-09-30 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | EGF-receptor specificity for phosphotyrosine-primed substrates provides signal integration with Src.
Nat.Struct.Mol.Biol., 22, 2015
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4LRM
 | | EGFR D770_N771insNPG in complex with PD168393 | | Descriptor: | Epidermal growth factor receptor, N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}propanamide | | Authors: | Yun, C.H, Eck, M.J. | | Deposit date: | 2013-07-20 | | Release date: | 2014-01-15 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3.526 Å) | | Cite: | Structural, Biochemical, and Clinical Characterization of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations in Lung Cancer.
Sci Transl Med, 5, 2013
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4LL0
 | | EGFR L858R/T790M in complex with PD168393 | | Descriptor: | Epidermal growth factor receptor, N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}propanamide | | Authors: | Yun, C.H, Eck, M.J. | | Deposit date: | 2013-07-09 | | Release date: | 2013-09-11 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (4 Å) | | Cite: | Mechanism for activation of mutated epidermal growth factor receptors in lung cancer.
Proc.Natl.Acad.Sci.USA, 110, 2013
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6P8Q
 | | EGFR in complex with a dihydrodibenzodiazepinone allosteric inhibitor. | | Descriptor: | 1,2-ETHANEDIOL, 10-benzyl-2-fluoro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one, ADENOSINE MONOPHOSPHATE, ... | | Authors: | Yun, C.H, Heppner, D.E, Eck, M.J. | | Deposit date: | 2019-06-07 | | Release date: | 2019-12-18 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.
Acs Med.Chem.Lett., 10, 2019
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5X2A
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5J87
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5X2F
 | | Crystal structure of EGFR 696-1022 T790M/V948R in complex with SKLB(6) | | Descriptor: | 9-cyclohexyl-N2-[4-(4-methylpiperazin-1-yl)phenyl]-N8-phenyl-purine-2,8-diamine, Epidermal growth factor receptor | | Authors: | Yun, C.H. | | Deposit date: | 2017-01-31 | | Release date: | 2018-02-07 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structural insights into drug development strategy targeting EGFR T790M/C797S.
Oncotarget, 9, 2018
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5X2C
 | | Crystal structure of EGFR 696-1022 T790M/V948R in complex with SKLB(5) | | Descriptor: | 1,2-ETHANEDIOL, 9-cyclopentyl-N2-[4-(4-methylpiperazin-1-yl)phenyl]-N8-phenyl-purine-2,8-diamine, CHLORIDE ION, ... | | Authors: | Yun, C.H. | | Deposit date: | 2017-01-31 | | Release date: | 2018-02-21 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Structural insights into drug development strategy targeting EGFR T790M/C797S.
Oncotarget, 9, 2018
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5X28
 | | Crystal structure of EGFR 696-1022 L858R in complex with SKLB(6) | | Descriptor: | 9-cyclohexyl-N2-[4-(4-methylpiperazin-1-yl)phenyl]-N8-phenyl-purine-2,8-diamine, CHLORIDE ION, Epidermal growth factor receptor | | Authors: | Yun, C.H. | | Deposit date: | 2017-01-31 | | Release date: | 2018-02-07 | | Last modified: | 2024-03-20 | | Method: | X-RAY DIFFRACTION (2.952 Å) | | Cite: | Structural insights into drug development strategy targeting EGFR T790M/C797S.
Oncotarget, 9, 2018
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5X27
 | | Crystal structure of EGFR 696-1022 L858R in complex with SKLB(5) | | Descriptor: | 9-cyclopentyl-N2-[4-(4-methylpiperazin-1-yl)phenyl]-N8-phenyl-purine-2,8-diamine, CHLORIDE ION, Epidermal growth factor receptor | | Authors: | Yun, C.H. | | Deposit date: | 2017-01-31 | | Release date: | 2018-02-07 | | Last modified: | 2024-03-20 | | Method: | X-RAY DIFFRACTION (2.952 Å) | | Cite: | Structural insights into drug development strategy targeting EGFR T790M/C797S.
Oncotarget, 9, 2018
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5X26
 | | Crystal structure of EGFR 696-1022 L858R in complex with SKLB(3) | | Descriptor: | CHLORIDE ION, Epidermal growth factor receptor, N2-[4-(4-methylpiperazin-1-yl)phenyl]-N8-phenyl-9-propan-2-yl-purine-2,8-diamine | | Authors: | Yun, C.H. | | Deposit date: | 2017-01-31 | | Release date: | 2018-02-07 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.951 Å) | | Cite: | Structural insights into drug development strategy targeting EGFR T790M/C797S.
Oncotarget, 9, 2018
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3IKA
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8IZP
 | | Multidrug resistance-associated protein 3 | | Descriptor: | ATP-binding cassette sub-family C member 3 | | Authors: | Yun, C.H, Gao, H.M. | | Deposit date: | 2023-04-07 | | Release date: | 2024-04-10 | | Method: | ELECTRON MICROSCOPY (3.31 Å) | | Cite: | structure of multidrug resistance-associated protein 3 at 3.31 Angstroms
To Be Published
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8IZR
 | | Multidrug resistance-associated protein 3 | | Descriptor: | ATP-binding cassette sub-family C member 2 | | Authors: | Yun, C.H, Gao, H.M. | | Deposit date: | 2023-04-07 | | Release date: | 2024-04-10 | | Method: | ELECTRON MICROSCOPY (3.62 Å) | | Cite: | structure of multidrug resistance-associated protein 2 at 3.62 Angstroms resolution
To Be Published
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7BTT
 | | A X-ray cocrystal structure of XMU-MP-5 bound to the ALK kinase domain | | Descriptor: | 2-(dimethylamino)-1-[5-methoxy-6-[[4-[(2-propan-2-ylsulfonylphenyl)amino]-5H-pyrrolo[3,2-d]pyrimidin-2-yl]amino]-2,3-dihydroindol-1-yl]ethanone, ALK tyrosine kinase receptor | | Authors: | Yun, C.H, Zhu, S.J. | | Deposit date: | 2020-04-02 | | Release date: | 2021-04-07 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (1.86 Å) | | Cite: | A X-ray cocrystal structure of XMU-MP-5 bound to the ALK kinase domain
To Be Published
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4LQM
 | | EGFR L858R in complex with PD168393 | | Descriptor: | CHLORIDE ION, Epidermal growth factor receptor, N-[4-(3-BROMO-PHENYLAMINO)-QUINAZOLIN-6-YL]-ACRYLAMIDE | | Authors: | Yun, C.H, Eck, M.J. | | Deposit date: | 2013-07-19 | | Release date: | 2014-01-15 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structural, Biochemical, and Clinical Characterization of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations in Lung Cancer.
Sci Transl Med, 5, 2013
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2J5E
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2J5F
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2ITZ
 | | Crystal structure of EGFR kinase domain L858R mutation in complex with Iressa | | Descriptor: | CHLORIDE ION, 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 (2.8 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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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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2JIV
 | | Crystal structure of EGFR kinase domain T790M mutation in compex with HKI-272 | | Descriptor: | CHLORIDE ION, EPIDERMAL GROWTH FACTOR RECEPTOR, N-(4-{[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino}-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)butanamide | | Authors: | Yun, C.-H, Mengwasser, K.E, Toms, A.V, Li, Y, Woo, M.S, Greulich, H, Wong, K.-K, Meyerson, M, Eck, M.J. | | Deposit date: | 2007-07-02 | | Release date: | 2008-01-22 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (3.5 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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