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7TVD
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Crystal structure of the kinase domain of EGFR exon-19 (del-747-749) mutant
分子名称: Epidermal growth factor receptor
著者Ashtekar, K.D, Stayrook, S.E, Lemmon, M.A.
登録日2022-02-04
公開日2022-02-16
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.96 Å)
主引用文献Biochemical and structural basis for differential inhibitor sensitivity of EGFR with distinct exon 19 mutations.
Nat Commun, 13, 2022
7TNH
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BU of 7tnh by Molmil
Crystal structure of CSF1R kinase domain in complex with DP-6233
分子名称: 2,2-dimethyl-N-[(6-methyl-5-{[2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl]oxy}pyridin-2-yl)carbamoyl]propanamide, CHLORIDE ION, Macrophage colony-stimulating factor 1 receptor,Fibroblast growth factor receptor 1 chimera, ...
著者Edwards, T.E, Arakaki, T.L, Chun, L, Flynn, D.L.
登録日2022-01-21
公開日2022-08-24
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.
Bioorg.Med.Chem.Lett., 74, 2022
7TEU
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BU of 7teu by Molmil
Crystal structure of JAK2 JH1 with type II inhibitor YLIU-04-105-1
分子名称: 3-{(4S)-2-[(cyclopropanecarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}-N-{3-[(4-ethylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl}-4-methylbenzamide, GLYCEROL, Tyrosine-protein kinase JAK2
著者Hubbard, S.R.
登録日2022-01-05
公開日2023-06-21
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (1.45 Å)
主引用文献New scaffolds for type II JAK2 inhibitors overcome the acquired G993A resistance mutation.
Cell Chem Biol, 30, 2023
7T6F
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BU of 7t6f by Molmil
Structure of active Janus Kinase (JAK) dimer complexed with cytokine receptor intracellular domain
分子名称: ADENOSINE, ADENOSINE-5'-DIPHOSPHATE, Interferon lambda receptor 1, ...
著者Glassman, C.R, Tsutsumi, N, Jude, K.M, Garcia, K.C.
登録日2021-12-13
公開日2022-03-16
最終更新日2024-02-28
実験手法ELECTRON MICROSCOPY (3.6 Å)
主引用文献Structure of a Janus kinase cytokine receptor complex reveals the basis for dimeric activation.
Science, 376, 2022
7T4J
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BU of 7t4j by Molmil
Crystal Structure of EGFR_D770_N771insNPG/V948R in complex with TAK-788
分子名称: 1,2-ETHANEDIOL, CITRIC ACID, Epidermal growth factor receptor, ...
著者Skene, R.J, Lane, W, Hu, Y.
登録日2021-12-10
公開日2022-12-07
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Bioorg.Med.Chem.Lett., 80, 2022
7T4I
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BU of 7t4i by Molmil
Crystal Structure of wild type EGFR in complex with TAK-788
分子名称: Epidermal growth factor receptor, propan-2-yl 2-[[4-[2-(dimethylamino)ethyl-methyl-amino]-2-methoxy-5-(propanoylamino)phenyl]amino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate
著者Skene, R.J, Lane, W.
登録日2021-12-10
公開日2022-12-07
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.61 Å)
主引用文献Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Bioorg.Med.Chem.Lett., 80, 2022
7T1T
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BU of 7t1t by Molmil
JAK2 JH2 IN COMPLEX WITH JAK292
分子名称: (2S)-2-[({4-[(2-amino-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy]phenyl}carbamoyl)amino]-4-phenylbutanoic acid, GLYCEROL, Tyrosine-protein kinase JAK2
著者Ippolito, J.A, Henry, S, Krimmer, S.G, Schlessinger, J, Jorgensen, W.L.
登録日2021-12-02
公開日2022-05-25
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.08 Å)
主引用文献Conversion of a False Virtual Screen Hit into Selective JAK2 JH2 Domain Binders Using Convergent Design Strategies
Acs Med.Chem.Lett., 13, 2022
7T0P
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BU of 7t0p by Molmil
JAK2 JH2 IN COMPLEX WITH JAK315
分子名称: 4'-{[5-amino-3-(4-sulfamoylanilino)-1H-1,2,4-triazole-1-carbonyl]amino}-4-(benzyloxy)[1,1'-biphenyl]-3-carboxylic acid, GLYCEROL, Tyrosine-protein kinase JAK2
著者Ippolito, J.A, Liosi, M.-E, Krimmer, S.G, Schlessinger, J, Jorgensen, W.L.
登録日2021-11-30
公開日2022-06-15
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.04 Å)
主引用文献Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
J.Med.Chem., 65, 2022
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
7SZ5
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BU of 7sz5 by Molmil
Cryo-EM structure of the extracellular module of the full-length EGFR bound to TGF-alpha "tips-separated" 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2021-12-22
実験手法ELECTRON MICROSCOPY (3.6 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
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
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
7SYD
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BU of 7syd by Molmil
Cryo-EM structure of the extracellular module of the full-length EGFR 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2021-11-24
公開日2021-12-22
実験手法ELECTRON MICROSCOPY (3.1 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
7STK
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BU of 7stk by Molmil
Full-length insulin receptor bound with unsaturated insulin WT (2 insulins bound) asymmetric conformation (Conformation 2)
分子名称: Insulin, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-11-14
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (4 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7STJ
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BU of 7stj by Molmil
Full-length insulin receptor bound with unsaturated insulin WT (2 insulins bound) asymmetric conformation (Conformation 1)
分子名称: Insulin, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-11-14
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (4.4 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7STI
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BU of 7sti by Molmil
Full-length insulin receptor bound with unsaturated insulin WT (1 insulin bound) asymmetric conformation
分子名称: Insulin, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-11-13
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (4.9 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7STH
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BU of 7sth by Molmil
Full-length insulin receptor bound with unsaturated insulin WT (2 insulin bound) symmetric conformation
分子名称: Insulin, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-11-13
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (3.5 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7SL7
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BU of 7sl7 by Molmil
Full-length insulin receptor bound with both site 1 binding deficient mutant insulin (A-V3E) and site 2 binding deficient mutant insulin (A-L13R)
分子名称: Insulin A chain (L13R), Insulin A chain (V3E), Insulin B chain, ...
著者Bai, X.C, Choi, E.
登録日2021-10-22
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (3.1 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7SL6
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BU of 7sl6 by Molmil
Full-length insulin receptor bound with site 2 binding deficient mutant insulin (B-L17R) -- symmetric conformation
分子名称: Insulin A chain, Insulin B chain, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-10-22
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (3.7 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7SL4
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BU of 7sl4 by Molmil
Full-length insulin receptor bound with site 2 binding deficient mutant insulin (B-L17R) -- asymmetric conformation
分子名称: Insulin A chain, Insulin B chain, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-10-22
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (5 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7SL3
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BU of 7sl3 by Molmil
Full-length insulin receptor bound with site 2 binding deficient mutant insulin (A-L13R) -- symmetric conformation
分子名称: Insulin A chain, Insulin B chain, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-10-22
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (3.4 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7SL2
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BU of 7sl2 by Molmil
Full-length insulin receptor bound with site 2 binding deficient mutant insulin (A-L13R) -- asymmetric conformation
分子名称: Insulin A chain, Insulin B chain, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-10-22
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (3.6 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7SL1
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BU of 7sl1 by Molmil
Full-length insulin receptor bound with site 1 binding deficient mutant insulin (A-V3E)
分子名称: Insulin A chain, Insulin B chain, Insulin receptor
著者Bai, X.C, Choi, E.
登録日2021-10-22
公開日2022-03-30
最終更新日2022-04-27
実験手法ELECTRON MICROSCOPY (3.4 Å)
主引用文献Synergistic activation of the insulin receptor via two distinct sites.
Nat.Struct.Mol.Biol., 29, 2022
7SI1
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BU of 7si1 by Molmil
Crystal structure of apo EGFR kinase domain
分子名称: 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Epidermal growth factor receptor, SULFATE ION
著者Kung, J.E, Wu, P, Kiefer, J.R, Sudhamsu, J.
登録日2021-10-12
公開日2022-10-26
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (1.6 Å)
主引用文献Clearing the Path to Rapid High-Quality Protein Purification
To Be Published

222415

件を2024-07-10に公開中

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