6WXN
 
 | | EGFR(T790M/V948R) in complex with LN3844 | | 分子名称: | CHLORIDE ION, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Heppner, D.E, Eck, M.J. | | 登録日 | 2020-05-11 | | 公開日 | 2021-05-19 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.76 Å) | | 主引用文献 | 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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6XL4
 | | EGFR(T790M/V948R) in complex with AZD9291 and DDC4002 | | 分子名称: | 10-benzyl-8-fluoro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one, Epidermal growth factor receptor, MAGNESIUM ION, ... | | 著者 | Heppner, D.E, Beyett, T.S, Eck, M.J. | | 登録日 | 2020-06-28 | | 公開日 | 2021-06-30 | | 最終更新日 | 2024-11-06 | | 実験手法 | X-RAY DIFFRACTION (2.06 Å) | | 主引用文献 | Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors.
Nat Commun, 13, 2022
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2F31
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3IKA
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2ITO
 | | 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
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2IUH
 | | Crystal structure of the PI3-kinase p85 N-terminal SH2 domain in complex with c-Kit phosphotyrosyl peptide | | 分子名称: | C-KIT PHOSPHOTYROSYL PEPTIDE, PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY ALPHA SUBUNIT | | 著者 | Nolte, R.T, Eck, M.J, Schlessinger, J, Shoelson, S.E, Harrison, S.C. | | 登録日 | 2006-06-03 | | 公開日 | 2006-06-06 | | 最終更新日 | 2021-04-28 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Crystal Structure of the Pi 3-Kinase P85 Amino-Terminal Sh2 Domain and its Phosphopeptide Complexes
Nat.Struct.Biol., 3, 1996
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2IUG
 | | Crystal structure of the PI3-kinase p85 N-terminal SH2 domain | | 分子名称: | PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY ALPHA SUBUNIT | | 著者 | Nolte, R.T, Eck, M.J, Schlessinger, J, Shoelson, S.E, Harrison, S.C. | | 登録日 | 2006-06-03 | | 公開日 | 2006-06-06 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.89 Å) | | 主引用文献 | Crystal Structure of the Pi 3-Kinase P85 Amino-Terminal Sh2 Domain and its Phosphopeptide Complexes
Nat.Struct.Biol., 3, 1996
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2IUI
 | | Crystal structure of the PI3-kinase p85 N-terminal SH2 domain in complex with PDGFR phosphotyrosyl peptide | | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Platelet-derived growth factor receptor beta | | 著者 | Nolte, R.T, Eck, M.J, Schlessinger, J, Shoelson, S.E, Harrison, S.C. | | 登録日 | 2006-06-03 | | 公開日 | 2006-06-06 | | 最終更新日 | 2021-04-28 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Crystal Structure of the Pi 3-Kinase P85 Amino- Terminal Sh2 Domain and its Phosphopeptide Complexes
Nat.Struct.Biol., 3, 1996
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2J5E
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2ITU
 | | Crystal structure of EGFR kinase domain L858R mutation in complex with AFN941 | | 分子名称: | 1,2,3,4-Tetrahydrogen Staurosporine, EPIDERMAL GROWTH FACTOR RECEPTOR | | 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 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.8 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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5TX3
 | | Structure of Maternal Embryonic Leucine Zipper Kinase | | 分子名称: | 7-[(1S)-4-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-({3-[(pyrrolidin-1-yl)methyl]phenyl}amino)-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one, Maternal embryonic leucine zipper kinase | | 著者 | Li, Q, Seo, H.-S, Huang, H.-T, Gray, N.S, Dhe-Paganon, S, Eck, M.J. | | 登録日 | 2016-11-15 | | 公開日 | 2017-11-22 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | MELK is not necessary for the proliferation of basal-like breast cancer cells.
Elife, 6, 2017
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4IM2
 | | Structure of Tank-Binding Kinase 1 | | 分子名称: | CHLORIDE ION, N-(3-{[5-iodo-4-({3-[(thiophen-2-ylcarbonyl)amino]propyl}amino)pyrimidin-2-yl]amino}phenyl)pyrrolidine-1-carboxamide, Serine/threonine-protein kinase TBK1 | | 著者 | Tu, D, Eck, M.J. | | 登録日 | 2013-01-01 | | 公開日 | 2013-03-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.5001 Å) | | 主引用文献 | Structure and ubiquitination-dependent activation of TANK-binding kinase 1.
Cell Rep, 3, 2013
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4IM0
 | | Structure of Tank-Binding Kinase 1 | | 分子名称: | N-{3-[(5-cyclopropyl-2-{[3-(morpholin-4-ylmethyl)phenyl]amino}pyrimidin-4-yl)amino]propyl}cyclobutanecarboxamide, Serine/threonine-protein kinase TBK1 | | 著者 | Tu, D, Eck, M.J. | | 登録日 | 2013-01-01 | | 公開日 | 2013-03-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.4001 Å) | | 主引用文献 | Structure and ubiquitination-dependent activation of TANK-binding kinase 1.
Cell Rep, 3, 2013
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4IM3
 | | Structure of Tank-Binding Kinase 1 | | 分子名称: | CHLORIDE ION, MERCURY (II) ION, N-(3-{[5-iodo-4-({3-[(thiophen-2-ylcarbonyl)amino]propyl}amino)pyrimidin-2-yl]amino}phenyl)pyrrolidine-1-carboxamide, ... | | 著者 | Tu, D, Eck, M.J. | | 登録日 | 2013-01-01 | | 公開日 | 2013-03-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (3.342 Å) | | 主引用文献 | Structure and ubiquitination-dependent activation of TANK-binding kinase 1.
Cell Rep, 3, 2013
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5WIN
 | | JAK2 Pseudokinase in complex with JNJ7706621 | | 分子名称: | 4-({5-amino-1-[(2,6-difluorophenyl)carbonyl]-1H-1,2,4-triazol-3-yl}amino)benzenesulfonamide, Tyrosine-protein kinase JAK2 | | 著者 | Li, Q, Eck, M.J, Li, K, Park, E. | | 登録日 | 2017-07-19 | | 公開日 | 2018-08-01 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.38 Å) | | 主引用文献 | Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.
ACS Chem. Biol., 14, 2019
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5TWU
 | | Structure of Maternal Embryonic Leucine Zipper Kinase | | 分子名称: | Maternal embryonic leucine zipper kinase | | 著者 | Li, Q, Seo, H.-S, Huang, H.-T, Gray, N.S, Dhe-Paganon, S, Eck, M.J. | | 登録日 | 2016-11-14 | | 公開日 | 2017-11-22 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.603 Å) | | 主引用文献 | MELK is not necessary for the proliferation of basal-like breast cancer cells.
Elife, 6, 2017
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5WFN
 | | Revised model of leiomodin 2-mediated actin regulation (alternate refinement of PDB 4RWT) | | 分子名称: | Actin-5C, Leiomodin-2, MAGNESIUM ION, ... | | 著者 | Yurtsever, Z, Eck, M.J, Dominguez, R. | | 登録日 | 2017-07-12 | | 公開日 | 2017-08-30 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Crystal structure of leiomodin 2 in complex with actin: a structural and functional reexamination
Biophys.J., 113, 2017
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5WIJ
 | | JAK2 Pseudokinase in complex with NU6140 | | 分子名称: | 4-{[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino}-N,N-diethylbenzamide, Tyrosine-protein kinase JAK2 | | 著者 | Li, Q, Eck, M.J, Li, K, Park, E. | | 登録日 | 2017-07-19 | | 公開日 | 2018-08-01 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.04 Å) | | 主引用文献 | Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.
ACS Chem. Biol., 14, 2019
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5WIL
 | | JAK2 Pseudokinase in complex with AZD7762 | | 分子名称: | 5-(3-fluorophenyl)-N-[(3S)-3-piperidyl]-3-ureido-thiophene-2-carboxamide, Tyrosine-protein kinase JAK2 | | 著者 | Li, Q, Eck, M.J, Li, K, Park, E. | | 登録日 | 2017-07-19 | | 公開日 | 2018-08-01 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.
ACS Chem. Biol., 14, 2019
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5WIK
 | | JAK2 Pseudokinase in complex with BI-D1870 | | 分子名称: | (7R)-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydropteridin-6(5H)-one, Tyrosine-protein kinase JAK2 | | 著者 | Li, Q, Eck, M.J, Li, K, Park, E. | | 登録日 | 2017-07-19 | | 公開日 | 2018-08-01 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.
ACS Chem. Biol., 14, 2019
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5WIM
 | | JAK2 Pseudokinase in complex with AT9283 | | 分子名称: | 1-cyclopropyl-3-{3-[5-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl}urea, Tyrosine-protein kinase JAK2 | | 著者 | Li, Q, Eck, M.J, Li, K, Park, E. | | 登録日 | 2017-07-19 | | 公開日 | 2018-08-01 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | | 主引用文献 | Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.
ACS Chem. Biol., 14, 2019
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4L00
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4L01
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4LL0
 | | EGFR L858R/T790M in complex with PD168393 | | 分子名称: | Epidermal growth factor receptor, N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}propanamide | | 著者 | Yun, C.H, Eck, M.J. | | 登録日 | 2013-07-09 | | 公開日 | 2013-09-11 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (4 Å) | | 主引用文献 | Mechanism for activation of mutated epidermal growth factor receptors in lung cancer.
Proc.Natl.Acad.Sci.USA, 110, 2013
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7KXZ
 | | Active conformation of EGFR kinase in complex with BI-4020 | | 分子名称: | (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, CHLORIDE ION, Epidermal growth factor receptor | | 著者 | Beyett, T.S, Eck, M.J. | | 登録日 | 2020-12-06 | | 公開日 | 2022-01-19 | | 最終更新日 | 2024-05-29 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structural Analysis of the Macrocyclic Inhibitor BI-4020 Binding to EGFR Kinase.
Chemmedchem, 2024
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