8OW3
 
 | | Crystal structure of wild-type c-MET bound by compound 2 | | Descriptor: | 5-[3,5-bis(fluoranyl)phenyl]-1-[(1S)-1-phenylethyl]pyrimidine-2,4-dione, Hepatocyte growth factor receptor | | Authors: | Collie, G.W. | | Deposit date: | 2023-04-26 | | Release date: | 2023-07-05 | | Last modified: | 2023-07-26 | | Method: | X-RAY DIFFRACTION (2.27 Å) | | Cite: | Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J.Med.Chem., 66, 2023
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8OWG
 | | Crystal structure of D1228V c-MET bound by compound 2 | | Descriptor: | 5-[3,5-bis(fluoranyl)phenyl]-1-[(1S)-1-phenylethyl]pyrimidine-2,4-dione, Hepatocyte growth factor receptor | | Authors: | Collie, G.W. | | Deposit date: | 2023-04-27 | | Release date: | 2023-07-05 | | Last modified: | 2023-07-26 | | Method: | X-RAY DIFFRACTION (2.631 Å) | | Cite: | Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J.Med.Chem., 66, 2023
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5FLF
 | | DISEASE LINKED MUTATION IN FGFR | | Descriptor: | ACETATE ION, CHLORIDE ION, FIBROBLAST GROWTH FACTOR RECEPTOR 1, ... | | Authors: | Thiyagarajan, N, Bunney, T.D, Katan, M. | | Deposit date: | 2015-10-26 | | Release date: | 2016-03-30 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.58 Å) | | Cite: | Landscape of Activating Cancer Mutations in Fgfr Kinases and Their Differential Responses to Inhibitors in Clinical Use.
Oncotarget, 7, 2016
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5FSI
 | | MTH1 substrate recognition: Complex with 8-oxo-dGTP. | | Descriptor: | 7,8-DIHYDRO-8-OXOGUANINE TRIPHOSPHATASE, 8-OXO-2'-DEOXYGUANOSINE-5'-TRIPHOSPHATE | | Authors: | Nissink, J.W.M, Bista, M, Breed, J, Carter, N, Embrey, K, Read, J, Phillips, C, Winter, J.J. | | Deposit date: | 2016-01-06 | | Release date: | 2016-07-11 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.63 Å) | | Cite: | Mth1 Substrate Recognition--an Example of Specific Promiscuity.
Plos One, 11, 2016
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4M14
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4M13
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4M12
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4M0Z
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4M15
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4M0Y
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2BYG
 | | 2nd PDZ Domain of Discs Large Homologue 2 | | Descriptor: | CHANNEL ASSOCIATED PROTEIN OF SYNAPSE-110 | | Authors: | Elkins, J.M, Schoch, G.A, Smee, C.E.A, Berridge, G, Salah, E, Sundstrom, M, Edwards, A, Arrowsmith, C, Weigelt, J, Doyle, D.A, Structural Genomics Consortium (SGC) | | Deposit date: | 2005-08-01 | | Release date: | 2005-08-04 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Structure of Pick1 and Other Pdz Domains Obtained with the Help of Self-Binding C-Terminal Extensions.
Protein Sci., 16, 2007
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5FXR
 | | IGFR-1R complex with a pyrimidine inhibitor. | | Descriptor: | 5-chloranyl-4-imidazo[1,2-a]pyridin-3-yl-N-(3-methyl-1-piperidin-4-yl-pyrazol-4-yl)pyrimidin-2-amine, INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR | | Authors: | Degorce, S, Boyd, S, Curwen, J, Ducray, R, Halsall, C, Jones, C, Lach, F, Lenz, E, Pass, M, Pass, S, Trigwell, C, Norman, R, Phillips, C. | | Deposit date: | 2016-03-02 | | Release date: | 2016-10-19 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).
J. Med. Chem., 59, 2016
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5FXS
 | | IGFR-1R complex with a pyrimidine inhibitor. | | Descriptor: | 2-[4-[4-[[(6Z)-5-chloranyl-6-pyrazolo[1,5-a]pyridin-3-ylidene-1H-pyrimidin-2-yl]amino]-3,5-dimethyl-pyrazol-1-yl]piperidin-1-yl]-N,N-dimethyl-ethanamide, ACETATE ION, INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR | | Authors: | Degorce, S, Boyd, S, Curwen, J, Ducray, R, Halsall, C, Jones, C, Lach, F, Lenz, E, Pass, M, Pass, S, Trigwell, C, Norman, R, Phillips, C. | | Deposit date: | 2016-03-02 | | Release date: | 2016-10-19 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).
J. Med. Chem., 59, 2016
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5FXQ
 | | IGFR-1R complex with a pyrimidine inhibitor. | | Descriptor: | 5-chloranyl-4-imidazo[1,2-a]pyridin-3-yl-N-(5-methyl-1-piperidin-4-yl-pyrazol-4-yl)pyrimidin-2-amine, INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR | | Authors: | Degorce, S, Boyd, S, Curwen, J, Ducray, R, Halsall, C, Jones, C, Lach, F, Lenz, E, Pass, M, Pass, S, Trigwell, C, Norman, R, Phillips, C. | | Deposit date: | 2016-03-02 | | Release date: | 2016-10-19 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).
J. Med. Chem., 59, 2016
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8G3K
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8G4F
 | | KRAS G12V complex with GDP imaged on a cryo-EM imaging scaffold | | Descriptor: | GTPase KRas, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Castells-Graells, R, Sawaya, M.R, Yeates, T.O. | | Deposit date: | 2023-02-09 | | Release date: | 2023-08-09 | | Last modified: | 2023-09-27 | | Method: | ELECTRON MICROSCOPY (2.91 Å) | | Cite: | Cryo-EM structure determination of small therapeutic protein targets at 3 angstrom -resolution using a rigid imaging scaffold.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8G42
 | | KRAS G12C complex with GDP imaged on a cryo-EM imaging scaffold | | Descriptor: | GTPase KRas, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Castells-Graells, R, Sawaya, M.R, Yeates, T.O. | | Deposit date: | 2023-02-08 | | Release date: | 2023-08-09 | | Last modified: | 2023-09-27 | | Method: | ELECTRON MICROSCOPY (3.02 Å) | | Cite: | Cryo-EM structure determination of small therapeutic protein targets at 3 angstrom -resolution using a rigid imaging scaffold.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8G47
 | | KRAS G12C complex with GDP and AMG 510 imaged on a cryo-EM imaging scaffold | | Descriptor: | AMG 510 (bound form), GTPase KRas, GUANOSINE-5'-DIPHOSPHATE, ... | | Authors: | Castells-Graells, R, Sawaya, M.R, Yeates, T.O. | | Deposit date: | 2023-02-08 | | Release date: | 2023-08-09 | | Last modified: | 2023-09-27 | | Method: | ELECTRON MICROSCOPY (3.19 Å) | | Cite: | Cryo-EM structure determination of small therapeutic protein targets at 3 angstrom -resolution using a rigid imaging scaffold.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8G4E
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8G4H
 | | KRAS G13C complex with GDP imaged on a cryo-EM imaging scaffold | | Descriptor: | GTPase KRas, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Castells-Graells, R, Sawaya, M.R, Yeates, T.O. | | Deposit date: | 2023-02-09 | | Release date: | 2023-08-09 | | Last modified: | 2023-09-27 | | Method: | ELECTRON MICROSCOPY (2.87 Å) | | Cite: | Cryo-EM structure determination of small therapeutic protein targets at 3 angstrom -resolution using a rigid imaging scaffold.
Proc.Natl.Acad.Sci.USA, 120, 2023
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5EW8
 | | FIBROBLAST GROWTH FACTOR RECEPTOR 1 IN COMPLEX WITH JNJ-4275693 | | Descriptor: | Fibroblast growth factor receptor 1, SULFATE ION, ~{N}'-(3,5-dimethoxyphenyl)-~{N}'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-~{N}-propan-2-yl-ethane-1,2-diamine | | Authors: | Ogg, D, Breed, J. | | Deposit date: | 2015-11-20 | | Release date: | 2016-03-30 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.63 Å) | | Cite: | Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use.
Oncotarget, 7, 2016
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4BU2
 | | 60S ribosomal protein L27A histidine hydroxylase (MINA53) in complex with Ni(II) and 2-oxoglutarate (2OG) | | Descriptor: | 1,2-ETHANEDIOL, 2-OXOGLUTARIC ACID, BIFUNCTIONAL LYSINE-SPECIFIC DEMETHYLASE AND HISTIDYL-HYDROXYLASE MINA, ... | | Authors: | Chowdhury, R, Clifton, I.J, McDonough, M.A, Ng, S.S, Pilka, E, Oppermann, U, Schofield, C.J. | | Deposit date: | 2013-06-19 | | Release date: | 2014-05-14 | | Last modified: | 2019-02-06 | | Method: | X-RAY DIFFRACTION (2.78 Å) | | Cite: | Ribosomal oxygenases are structurally conserved from prokaryotes to humans.
Nature, 510, 2014
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4CCJ
 | | 60S ribosomal protein L8 histidine hydroxylase (NO66) in apo form | | Descriptor: | 1,2-ETHANEDIOL, BIFUNCTIONAL LYSINE-SPECIFIC DEMETHYLASE AND HISTIDYL-HYDROXYLASE NO66 | | Authors: | Chowdhury, R, Ge, W, Clifton, I.J, Schofield, C.J. | | Deposit date: | 2013-10-23 | | Release date: | 2014-05-14 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Ribosomal oxygenases are structurally conserved from prokaryotes to humans.
Nature, 510, 2014
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4CCO
 | | 60S ribosomal protein L8 histidine hydroxylase (NO66 S373C) in complex with Mn(II), N-oxalylglycine (NOG) and 60S ribosomal protein L8 (RPL8 G214C) peptide fragment (complex-3) | | Descriptor: | 1,2-ETHANEDIOL, 60S RIBOSOMAL PROTEIN L8, BIFUNCTIONAL LYSINE-SPECIFIC DEMETHYLASE AND HISTIDYL-HYDROXYLASE NO66, ... | | Authors: | Chowdhury, R, Schofield, C.J. | | Deposit date: | 2013-10-23 | | Release date: | 2014-05-14 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Ribosomal oxygenases are structurally conserved from prokaryotes to humans.
Nature, 510, 2014
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4CCM
 | | 60S ribosomal protein L8 histidine hydroxylase (NO66) in complex with Mn(II), N-oxalylglycine (NOG) and 60S ribosomal protein L8 (RPL8 G220C) peptide fragment (complex-1) | | Descriptor: | 1,2-ETHANEDIOL, 60S RIBOSOMAL PROTEIN L8, BIFUNCTIONAL LYSINE-SPECIFIC DEMETHYLASE AND HISTIDYL-HYDROXYLASE NO66, ... | | Authors: | Chowdhury, R, Schofield, C.J. | | Deposit date: | 2013-10-23 | | Release date: | 2014-05-14 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.51 Å) | | Cite: | Ribosomal oxygenases are structurally conserved from prokaryotes to humans.
Nature, 510, 2014
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