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
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7TYM
 | | Cryo-EM Structure of insulin receptor-related receptor (IRR) in active-state captured at pH 9. The 3D refinement was applied with C2 symmetry | | Descriptor: | Insulin receptor-related protein | | Authors: | Wang, L.W, Hall, C, Li, J, Choi, E, Bai, X.C. | | Deposit date: | 2022-02-13 | | Release date: | 2023-02-15 | | Last modified: | 2023-05-31 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Structural basis of the alkaline pH-dependent activation of insulin receptor-related receptor.
Nat.Struct.Mol.Biol., 30, 2023
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7TYK
 | | Cryo-EM Structure of insulin receptor-related receptor (IRR) in apo-state captured at pH 7. The 3D refinement was applied with C2 symmetry | | Descriptor: | Insulin receptor-related protein | | Authors: | Wang, L.W, Hall, C, Li, J, Choi, E, Bai, X.C. | | Deposit date: | 2022-02-13 | | Release date: | 2023-02-15 | | Last modified: | 2023-05-31 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structural basis of the alkaline pH-dependent activation of insulin receptor-related receptor.
Nat.Struct.Mol.Biol., 30, 2023
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7TYJ
 | | Cryo-EM Structure of insulin receptor-related receptor (IRR) in apo-state captured at pH 7. The 3D refinement was focused on one of two halves with C1 symmetry applied | | Descriptor: | Insulin receptor-related protein | | Authors: | Wang, L.W, Hall, C, Li, J, Choi, E, Bai, X.C. | | Deposit date: | 2022-02-13 | | Release date: | 2023-02-15 | | Last modified: | 2023-05-31 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Structural basis of the alkaline pH-dependent activation of insulin receptor-related receptor.
Nat.Struct.Mol.Biol., 30, 2023
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7TVD
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7TNH
 | | Crystal structure of CSF1R kinase domain in complex with DP-6233 | | Descriptor: | 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, ... | | Authors: | Edwards, T.E, Arakaki, T.L, Chun, L, Flynn, D.L. | | Deposit date: | 2022-01-21 | | Release date: | 2022-08-24 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.
Bioorg.Med.Chem.Lett., 74, 2022
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7TEU
 | | Crystal structure of JAK2 JH1 with type II inhibitor YLIU-04-105-1 | | Descriptor: | 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 | | Authors: | Hubbard, S.R. | | Deposit date: | 2022-01-05 | | Release date: | 2023-06-21 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.45 Å) | | Cite: | New scaffolds for type II JAK2 inhibitors overcome the acquired G993A resistance mutation.
Cell Chem Biol, 30, 2023
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7T6F
 | | Structure of active Janus Kinase (JAK) dimer complexed with cytokine receptor intracellular domain | | Descriptor: | ADENOSINE, ADENOSINE-5'-DIPHOSPHATE, Interferon lambda receptor 1, ... | | Authors: | Glassman, C.R, Tsutsumi, N, Jude, K.M, Garcia, K.C. | | Deposit date: | 2021-12-13 | | Release date: | 2022-03-16 | | Last modified: | 2024-02-28 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | Structure of a Janus kinase cytokine receptor complex reveals the basis for dimeric activation.
Science, 376, 2022
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7T4J
 | | Crystal Structure of EGFR_D770_N771insNPG/V948R in complex with TAK-788 | | Descriptor: | 1,2-ETHANEDIOL, CITRIC ACID, Epidermal growth factor receptor, ... | | Authors: | Skene, R.J, Lane, W, Hu, Y. | | Deposit date: | 2021-12-10 | | Release date: | 2022-12-07 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | 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
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7T4I
 | | Crystal Structure of wild type EGFR in complex with TAK-788 | | Descriptor: | 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 | | Authors: | Skene, R.J, Lane, W. | | Deposit date: | 2021-12-10 | | Release date: | 2022-12-07 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.61 Å) | | Cite: | 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
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7T1T
 | | JAK2 JH2 IN COMPLEX WITH JAK292 | | Descriptor: | (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 | | Authors: | Ippolito, J.A, Henry, S, Krimmer, S.G, Schlessinger, J, Jorgensen, W.L. | | Deposit date: | 2021-12-02 | | Release date: | 2022-05-25 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.08 Å) | | Cite: | Conversion of a False Virtual Screen Hit into Selective JAK2 JH2 Domain Binders Using Convergent Design Strategies
Acs Med.Chem.Lett., 13, 2022
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7T0P
 | | JAK2 JH2 IN COMPLEX WITH JAK315 | | Descriptor: | 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 | | Authors: | Ippolito, J.A, Liosi, M.-E, Krimmer, S.G, Schlessinger, J, Jorgensen, W.L. | | Deposit date: | 2021-11-30 | | Release date: | 2022-06-15 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.04 Å) | | Cite: | Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
J.Med.Chem., 65, 2022
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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
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7SZ5
 | | Cryo-EM structure of the extracellular module of the full-length EGFR bound to TGF-alpha "tips-separated" 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: | 2021-12-22 | | Method: | ELECTRON MICROSCOPY (3.6 Å) | | Cite: | A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor.
Elife, 10, 2021
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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
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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
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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
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7SYD
 | | Cryo-EM structure of the extracellular module of the full-length EGFR 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: | 2021-11-24 | | Release date: | 2021-12-22 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor.
Elife, 10, 2021
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7STK
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7STJ
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7STI
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7STH
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7SL7
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7SL6
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7SL4
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