3RI1
 
 | | Crystal structure of the catalytic domain of FGFR2 kinase in complex with ARQ 069 | | Descriptor: | (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine, Fibroblast growth factor receptor 2, SULFATE ION | | Authors: | Eathiraj, S, Palma, R, Hirschi, M, Volckova, E, Nakuci, E, Castro, J, Chen, C.R, Chan, T.C, France, D.S, Ashwell, M.A. | | Deposit date: | 2011-04-12 | | Release date: | 2011-05-04 | | Last modified: | 2011-10-19 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.
J.Biol.Chem., 286, 2011
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3RHK
 | | Crystal structure of the catalytic domain of c-Met kinase in complex with ARQ 197 | | Descriptor: | 1-[(3R,4R)-4-(1H-indol-3-yl)-2,5-dioxopyrrolidin-3-yl]pyrrolo[3,2,1-ij]quinolinium, Hepatocyte growth factor receptor | | Authors: | Eathiraj, S, Palma, R, Volckova, E, Hirschi, M, France, D.S, Ashwell, M.A, Chan, T.C. | | Deposit date: | 2011-04-11 | | Release date: | 2011-04-27 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.94 Å) | | Cite: | Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation by ARQ 197.
J.Biol.Chem., 286, 2011
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3RHX
 | | Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069 | | Descriptor: | (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine, 1,2-ETHANEDIOL, Basic fibroblast growth factor receptor 1, ... | | Authors: | Eathiraj, S, Palma, R, Hirschi, M, Volckova, E, Nakuci, E, Castro, J, Chen, C.R, Chan, T.C, France, D.S, Ashwell, M.A. | | Deposit date: | 2011-04-12 | | Release date: | 2011-05-04 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.01 Å) | | Cite: | A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.
J.Biol.Chem., 286, 2011
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6L92
 | | A basket type G-quadruplex in WNT DNA promoter | | Descriptor: | DNA (5'-D(*GP*GP*GP*CP*CP*AP*CP*CP*GP*GP*GP*CP*AP*GP*TP*GP*GP*GP*CP*GP*GP*G)-3') | | Authors: | Wang, Z.F, Li, M.H, Chu, I.T, Winnerdy, F.R, Phan, A.T, Chang, T.C. | | Deposit date: | 2019-11-08 | | Release date: | 2019-12-11 | | Last modified: | 2024-05-15 | | Method: | SOLUTION NMR | | Cite: | Cytosine epigenetic modification modulates the formation of an unprecedented G4 structure in the WNT1 promoter.
Nucleic Acids Res., 48, 2020
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6L8M
 | | WNT DNA promoter mutant G-quadruplex | | Descriptor: | DNA (5'-D(*GP*GP*GP*TP*CP*AP*CP*CP*GP*GP*GP*CP*AP*GP*TP*GP*GP*GP*CP*GP*GP*G)-3') | | Authors: | Wang, Z.F, Li, M.H, Chu, I.T, Winnerdy, F.R, Phan, A.T, Chang, T.C. | | Deposit date: | 2019-11-06 | | Release date: | 2019-12-11 | | Last modified: | 2024-05-15 | | Method: | SOLUTION NMR | | Cite: | Cytosine epigenetic modification modulates the formation of an unprecedented G4 structure in the WNT1 promoter.
Nucleic Acids Res., 48, 2020
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4EJN
 | | Crystal structure of autoinhibited form of AKT1 in complex with N-(4-(5-(3-acetamidophenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-3-yl)benzyl)-3-fluorobenzamide | | Descriptor: | 1,2-ETHANEDIOL, 2-BUTANOL, N-(4-{5-[3-(acetylamino)phenyl]-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-3-yl}benzyl)-3-fluorobenzamide, ... | | Authors: | Eathiraj, S. | | Deposit date: | 2012-04-06 | | Release date: | 2012-05-23 | | Last modified: | 2013-01-02 | | Method: | X-RAY DIFFRACTION (2.19 Å) | | Cite: | Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.
J.Med.Chem., 55, 2012
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6NLH
 | | Structure of human triose phosphate isomerase R189A | | Descriptor: | BROMIDE ION, PHOSPHATE ION, SODIUM ION, ... | | Authors: | Richards, K.R, Roland, B.P, Palladino, M.J, VanDemark, A.P. | | Deposit date: | 2019-01-08 | | Release date: | 2019-06-19 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.199 Å) | | Cite: | Missense variant in TPI1 (Arg189Gln) causes neurologic deficits through structural changes in the triosephosphate isomerase catalytic site and reduced enzyme levels in vivo.
Biochim Biophys Acta Mol Basis Dis, 1865, 2019
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6O2L
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6FAX
 | | Complex of Human CD40 Ectodomain with Lob 7.4 Fab | | Descriptor: | Lob 7.4 heavy chain, Lob 7.4 light chain, Tumor necrosis factor receptor superfamily member 5 | | Authors: | Orr, C.M, Tews, I, Pearson, A.R. | | Deposit date: | 2017-12-18 | | Release date: | 2018-02-07 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.99 Å) | | Cite: | Complex Interplay between Epitope Specificity and Isotype Dictates the Biological Activity of Anti-human CD40 Antibodies.
Cancer Cell, 33, 2018
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8TH1
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8TH7
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8TH6
 | | Crystal Structure of the G3BP1 NTF2-like domain bound to USP10 peptide | | Descriptor: | 1,2-ETHANEDIOL, Ras GTPase-activating protein-binding protein 1, Ubiquitin carboxyl-terminal hydrolase 10 | | Authors: | Hughes, M.P, Taylor, J.P, Yang, Z. | | Deposit date: | 2023-07-14 | | Release date: | 2024-03-20 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.34 Å) | | Cite: | Interaction between host G3BP and viral nucleocapsid protein regulates SARS-CoV-2 replication and pathogenicity.
Cell Rep, 43, 2024
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8TH5
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6JJ0
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