8F7P
 
 | | BRAF kinase in complex with LXH254 (naporafenib) | | Descriptor: | N-{3-[2-(2-hydroxyethoxy)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl}-2-(trifluoromethyl)pyridine-4-carboxamide, Serine/threonine-protein kinase B-raf | | Authors: | Tkacik, E, Li, K, Gonzalez Del-Pino, G, Eck, M.J. | | Deposit date: | 2022-11-20 | | Release date: | 2023-04-12 | | Last modified: | 2024-05-22 | | Method: | X-RAY DIFFRACTION (2.74 Å) | | Cite: | Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib.
J.Biol.Chem., 299, 2023
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8F7O
 | | BRAF kinase in complex with TAK580 (tovorafenib) | | Descriptor: | 6-amino-5-chloro-N-[(1R)-1-(5-{[5-chloro-4-(trifluoromethyl)pyridin-2-yl]carbamoyl}-1,3-thiazol-2-yl)ethyl]pyrimidine-4-carboxamide, Serine/threonine-protein kinase B-raf | | Authors: | Tkacik, E, Li, K, Gonzalez Del-Pino, G, Eck, M.J. | | Deposit date: | 2022-11-20 | | Release date: | 2023-04-12 | | Last modified: | 2024-05-22 | | Method: | X-RAY DIFFRACTION (3.54 Å) | | Cite: | Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib.
J.Biol.Chem., 299, 2023
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8F1Z
 | | EGFR kinase in complex with Bayer #33 | | Descriptor: | (2P)-3-(3-chloro-2-methoxyanilino)-2-[3-(2-methoxy-2-methylpropoxy)pyridin-4-yl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one, CITRIC ACID, Epidermal growth factor receptor | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2022-11-06 | | Release date: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | EGFR kinase in complex with Bayer #33
To be published
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8F1Y
 | | EGFR kinase in complex with poziotinib | | Descriptor: | 1-[4-[4-[[3,4-bis(chloranyl)-2-fluoranyl-phenyl]amino]-7-methoxy-quinazolin-6-yl]oxypiperidin-1-yl]propan-1-one, CITRIC ACID, Epidermal growth factor receptor | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2022-11-06 | | Release date: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | EGFR kinase in complex with poziotinib
To be published
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8F1X
 | | EGFR kinase in complex with mobocertinib (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: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2022-11-06 | | Release date: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | EGFR kinase in complex with mobocertinib (TAK-788)
To be published
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8F1W
 | | EGFR(T790M/V948R) kinase in complex with poziotinib | | Descriptor: | 1-[4-[4-[[3,4-bis(chloranyl)-2-fluoranyl-phenyl]amino]-7-methoxy-quinazolin-6-yl]oxypiperidin-1-yl]propan-1-one, Epidermal growth factor receptor | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2022-11-06 | | Release date: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | EGFR(T790M/V948R) kinase in complex with poziotinib
To be published
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8F1H
 | | EGFR kinase in complex with TAS6417 (CLN-081) | | Descriptor: | CITRIC ACID, Epidermal growth factor receptor, N-[(5P,8S,10R)-4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl]prop-2-enamide | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2022-11-05 | | Release date: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | EGFR kinase in complex with TAS6417 (CLN-081)
To be published
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8EZ0
 | | Cryo-EM structure of 4 insulins bound full-length mouse IR mutant with physically decoupled alpha CTs (C684S/C685S/C687S; denoted as IR-3CS) Symmetric conformation | | Descriptor: | Insulin, Insulin receptor | | Authors: | Li, J, Wu, J.Y, Hall, C, Bai, X.C, Choi, E. | | Deposit date: | 2022-10-29 | | Release date: | 2022-11-09 | | Last modified: | 2023-08-30 | | Method: | ELECTRON MICROSCOPY (3.7 Å) | | Cite: | Molecular basis for the role of disulfide-linked alpha CTs in the activation of insulin-like growth factor 1 receptor and insulin receptor.
Elife, 11, 2022
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8EYY
 | | Cryo-EM structure of 4 insulins bound full-length mouse IR mutant with physically decoupled alpha CTs (C684S/C685S/C687S, denoted as IR-3CS) Asymmetric conformation 2 | | Descriptor: | Insulin, Insulin receptor | | Authors: | Li, J, Wu, J.Y, Hall, C, Bai, X.C, Choi, E. | | Deposit date: | 2022-10-29 | | Release date: | 2022-11-09 | | Last modified: | 2022-12-07 | | Method: | ELECTRON MICROSCOPY (4.9 Å) | | Cite: | Molecular basis for the role of disulfide-linked alpha CTs in the activation of insulin-like growth factor 1 receptor and insulin receptor.
Elife, 11, 2022
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8EYX
 | | Cryo-EM structure of 4 insulins bound full-length mouse IR mutant with physically decoupled alpha CTs (C684S/C685S/C687S; denoted as IR-3CS) Asymmetric conformation 1 | | Descriptor: | Insulin, Insulin receptor | | Authors: | Li, J, Wu, J.Y, Hall, C, Bai, X.C, Choi, E. | | Deposit date: | 2022-10-29 | | Release date: | 2022-11-09 | | Last modified: | 2022-12-07 | | Method: | ELECTRON MICROSCOPY (4.5 Å) | | Cite: | Molecular basis for the role of disulfide-linked alpha CTs in the activation of insulin-like growth factor 1 receptor and insulin receptor.
Elife, 11, 2022
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8EYR
 | | Cryo-EM structure of two IGF1 bound full-length mouse IGF1R mutant (four glycine residues inserted in the alpha-CT; IGF1R-P674G4): symmetric conformation | | Descriptor: | Insulin-like growth factor 1 receptor, Insulin-like growth factor I | | Authors: | Li, J, Wu, J.Y, Hall, C, Bai, X.C, Choi, E. | | Deposit date: | 2022-10-28 | | Release date: | 2022-11-09 | | Last modified: | 2022-12-07 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Molecular basis for the role of disulfide-linked alpha CTs in the activation of insulin-like growth factor 1 receptor and insulin receptor.
Elife, 11, 2022
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8EX2
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8EX1
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8EX0
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8EWY
 | | Structure of Janus Kinase (JAK) dimer complexed with cytokine receptor intracellular domain | | Descriptor: | ADENOSINE, ADENOSINE-5'-DIPHOSPHATE, Interferon lambda receptor 1, ... | | Authors: | Caveney, N.A, Saxton, R.A, Waghray, D, Garcia, K.C. | | Deposit date: | 2022-10-24 | | Release date: | 2023-03-08 | | Last modified: | 2023-03-22 | | Method: | ELECTRON MICROSCOPY (5.5 Å) | | Cite: | Structural basis of Janus kinase trans-activation.
Cell Rep, 42, 2023
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8EME
 | | EGFR(T790M/V948R) in complex with ZNL-0056 | | Descriptor: | 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 | | Authors: | Beyett, T.S, Eck, M.J. | | Deposit date: | 2022-09-27 | | Release date: | 2023-10-18 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (3.32 Å) | | Cite: | Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality
Acs Cent.Sci., 2024
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8EJB
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8E4T
 | | Crystal structure of the kinase domain of RTKC8 from the choanoflagellate Monosiga brevicollis | | Descriptor: | PHOSPHATE ION, RTKC8 Kinase domain, STAUROSPORINE | | Authors: | Bajaj, T, Gee, C.L, Kuriyan, J. | | Deposit date: | 2022-08-18 | | Release date: | 2023-06-21 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Crystal structure of the kinase domain of a receptor tyrosine kinase from a choanoflagellate, Monosiga brevicollis.
Plos One, 18, 2023
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8E2M
 | | Bruton's tyrosine kinase (BTK) with compound 13 | | Descriptor: | (5P)-5-[4-methyl-6-(2-methylpropyl)pyridin-3-yl]-4-oxo-N-[(1R,2S)-2-propanamidocyclopentyl]-4,5-dihydro-3H-1-thia-3,5,8-triazaacenaphthylene-2-carboxamide, TRIETHYLENE GLYCOL, Tyrosine-protein kinase BTK | | Authors: | Alexander, R, Milligan, C.M. | | Deposit date: | 2022-08-15 | | Release date: | 2022-11-16 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.904 Å) | | Cite: | Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
J.Med.Chem., 65, 2022
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8E1X
 | | FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine analog (Compound 29) | | Descriptor: | (5M)-N-methyl-5-{(6M,8S)-5-{[(3S)-oxolan-3-yl]amino}-6-[1-(propan-2-yl)-1H-pyrazol-3-yl]pyrazolo[1,5-a]pyrimidin-3-yl}pyridine-3-carboxamide, Fibroblast growth factor receptor 2 | | Authors: | Lei, H.-T, Epling, L.B, Deller, M.C. | | Deposit date: | 2022-08-11 | | Release date: | 2022-11-23 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.68 Å) | | Cite: | Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
J.Med.Chem., 65, 2022
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8DWN
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8DTM
 | | Cryo-EM structure of insulin receptor (IR) bound with S597 component 2 | | Descriptor: | Insulin mimetic peptide S597 component 2, Insulin receptor | | Authors: | Park, J, Li, J, Mayer, J.P, Ball, K.A, Wu, J.Y, Hall, C, Accili, D, Stowell, M.H.B, Bai, X.C, Choi, E. | | Deposit date: | 2022-07-26 | | Release date: | 2022-09-07 | | Last modified: | 2022-10-12 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Activation of the insulin receptor by an insulin mimetic peptide.
Nat Commun, 13, 2022
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8DTL
 | | Cryo-EM structure of insulin receptor (IR) bound with S597 peptide | | Descriptor: | Insulin mimetic peptide S597, Insulin receptor | | Authors: | Park, J, Li, J, Mayer, J.P, Ball, K.A, Wu, J.Y, Hall, C, Accili, D, Stowell, M.H.B, Bai, X.C, Choi, E. | | Deposit date: | 2022-07-25 | | Release date: | 2022-09-07 | | Last modified: | 2022-10-12 | | Method: | ELECTRON MICROSCOPY (5.4 Å) | | Cite: | Activation of the insulin receptor by an insulin mimetic peptide.
Nat Commun, 13, 2022
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8DSW
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8DSO
 | | Structure of cIAP1, BTK and BCCov | | Descriptor: | (4S)-4-[2-(2-{4-[(2E)-4-{(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl}-4-oxobut-2-en-1-yl]piperazin-1-yl}ethoxy)acetamido]-1-{(2S)-2-cyclohexyl-2-[(N-methyl-L-alanyl)amino]acetyl}-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-L-prolinamide bound form, Baculoviral IAP repeat-containing protein 2, Tyrosine-protein kinase BTK, ... | | Authors: | Schiemer, J.S, Calabrese, M.F. | | Deposit date: | 2022-07-22 | | Release date: | 2023-03-08 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.334 Å) | | Cite: | A covalent BTK ternary complex compatible with targeted protein degradation.
Nat Commun, 14, 2023
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