3M7F
| Crystal structure of the Nedd4 C2/Grb10 SH2 complex | Descriptor: | E3 ubiquitin-protein ligase NEDD4, Growth factor receptor-bound protein 10 | Authors: | Huang, Q, Szebenyi, M. | Deposit date: | 2010-03-16 | Release date: | 2010-10-27 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Structural Basis for the Interaction between the Growth Factor-binding Protein GRB10 and the E3 Ubiquitin Ligase NEDD4. J.Biol.Chem., 285, 2010
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3NHN
| Crystal structure of the SRC-family kinase HCK SH3-SH2-linker regulatory region | Descriptor: | Tyrosine-protein kinase HCK | Authors: | Alvarado, J.J, Betts, L, Moroco, J.A, Smithgall, T.E, Yeh, J.I. | Deposit date: | 2010-06-14 | Release date: | 2010-09-01 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.61 Å) | Cite: | Crystal Structure of the Src Family Kinase Hck SH3-SH2 Linker Regulatory Region Supports an SH3-dominant Activation Mechanism. J.Biol.Chem., 285, 2010
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4XEY
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4XZ1
| ZAP-70-tSH2:Compound-B adduct | Descriptor: | 2-[(7-chloro-4-nitro-2,1,3-benzoxadiazol-5-yl)amino]ethanol, Tyrosine-protein kinase ZAP-70, doubly phosphorylated ITAM peptide | Authors: | Barros, T, Kuriyan, J, Winger, J.A, Visperas, P.R. | Deposit date: | 2015-02-03 | Release date: | 2015-07-29 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Modification by covalent reaction or oxidation of cysteine residues in the tandem-SH2 domains of ZAP-70 and Syk can block phosphopeptide binding. Biochem. J., 465, 2015
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4Y5U
| Transcription factor | Descriptor: | NICKEL (II) ION, Signal transducer and activator of transcription 6 | Authors: | Li, J, Niu, F, Ouyang, S, Liu, Z. | Deposit date: | 2015-02-12 | Release date: | 2016-02-17 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.708 Å) | Cite: | Structural basis for DNA recognition by STAT6 Proc.Natl.Acad.Sci.USA, 113, 2016
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4Y5W
| Transcription factor-DNA complex | Descriptor: | DNA (5'-D(P*AP*TP*GP*GP*AP*TP*TP*TP*CP*CP*TP*AP*GP*GP*AP*AP*GP*AP*CP*AP*A)-3'), DNA (5'-D(P*TP*TP*GP*TP*CP*TP*TP*CP*CP*TP*AP*GP*GP*AP*AP*AP*TP*CP*CP*AP*T)-3'), Signal transducer and activator of transcription 6 | Authors: | Li, J, Niu, F, Ouyang, S, Liu, Z. | Deposit date: | 2015-02-12 | Release date: | 2016-02-17 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (3.104 Å) | Cite: | Structural basis for DNA recognition by STAT6 Proc.Natl.Acad.Sci.USA, 113, 2016
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7TVA
| Stat5a Core in complex with AK2292 | Descriptor: | DI(HYDROXYETHYL)ETHER, MALONATE ION, N-{5-[difluoro(phosphono)methyl]-1-benzothiophene-2-carbonyl}-3-methyl-L-valyl-L-prolyl-N-(5-{2-[(3R)-2,6-dioxopiperidin-3-yl]-1-oxo-2,3-dihydro-1H-isoindol-4-yl}pent-4-yn-1-yl)-N-methyl-N~3~-[4-(1,3-thiazol-2-yl)phenyl]-beta-alaninamide, ... | Authors: | Meagher, J.L, Stuckey, J.A. | Deposit date: | 2022-02-04 | Release date: | 2023-02-15 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.835 Å) | Cite: | A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo. Nat.Chem.Biol., 19, 2023
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7VXG
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4YKN
| Pi3K alpha lipid kinase with Active Site Inhibitor | Descriptor: | 3-(6-methoxypyridin-3-yl)-5-[({4-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfamoyl]phenyl}amino)methyl]benzoic acid, Phosphatidylinositol 3-kinase regulatory subunit alpha,Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform fusion protein | Authors: | Elkins, P.A. | Deposit date: | 2015-03-04 | Release date: | 2015-06-17 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Discovery of a Potent Class of PI3K alpha Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT). Acs Med.Chem.Lett., 6, 2015
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7UY3
| Crystal structure of human Fgr tyrosine kinase in complex with TL02-59 | Descriptor: | 1,2-ETHANEDIOL, 3-[(6,7-dimethoxyquinazolin-4-yl)oxy]-N-{4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-4-methylbenzamide, GLYCEROL, ... | Authors: | Du, S, Alvarado, J.J, Smithgall, T.E. | Deposit date: | 2022-05-06 | Release date: | 2022-12-28 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.99 Å) | Cite: | ATP-site inhibitors induce unique conformations of the acute myeloid leukemia-associated Src-family kinase, Fgr. Structure, 30, 2022
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7UY0
| Crystal structure of human Fgr tyrosine kinase in complex with A-419259 | Descriptor: | 7-[trans-4-(4-methylpiperazin-1-yl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, CHLORIDE ION, GLYCEROL, ... | Authors: | Du, S, Alvarado, J.J, Smithgall, T.E. | Deposit date: | 2022-05-06 | Release date: | 2022-12-28 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.55 Å) | Cite: | ATP-site inhibitors induce unique conformations of the acute myeloid leukemia-associated Src-family kinase, Fgr. Structure, 30, 2022
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8AM0
| Crystal structure of human T1061E PI3Kalpha in complex with its regulatory subunit and the inhibitor GDC-0077 (Inavolisib) | Descriptor: | (2R)-2-[[2-[(4S)-4-[bis(fluoranyl)methyl]-2-oxidanylidene-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide, 1,2-ETHANEDIOL, CHLORIDE ION, ... | Authors: | Goncalves, M, Johnson, J.L, Roewer, K.M. | Deposit date: | 2022-08-02 | Release date: | 2023-12-13 | Last modified: | 2024-01-03 | Method: | X-RAY DIFFRACTION (2.818 Å) | Cite: | Epinephrine inhibits PI3K alpha via the Hippo kinases. Cell Rep, 42, 2023
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3GQI
| Crystal Structure of activated receptor tyrosine kinase in complex with substrates | Descriptor: | Basic fibroblast growth factor receptor 1, DECAVANADATE, MAGNESIUM ION, ... | Authors: | Bae, J.H, Lew, E.D, Yuzawa, S, Tome, F, Lax, I, Schlessinger, J. | Deposit date: | 2009-03-24 | Release date: | 2009-08-18 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site. Cell(Cambridge,Mass.), 138, 2009
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1X27
| Crystal Structure of Lck SH2-SH3 with SH2 binding site of p130Cas | Descriptor: | CRK-associated substrate, Proto-oncogene tyrosine-protein kinase LCK, SODIUM ION | Authors: | Nasertorabi, F, Tars, K, Becherer, K, Kodandapani, R, Liljas, L, Vuori, K, Ely, K.R. | Deposit date: | 2005-04-20 | Release date: | 2006-02-07 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Molecular basis for regulation of Src by the docking protein p130Cas J.MOL.RECOG., 19, 2006
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4OHI
| LEOPARD Syndrome-Associated SHP2/Q510E mutant | Descriptor: | Tyrosine-protein phosphatase non-receptor type 11 | Authors: | Yu, Z.H, Zhang, R.Y, Walls, C.D, Chen, L, Zhang, S, Wu, L, Wang, L, Liu, S, Zhang, Z.Y. | Deposit date: | 2014-01-17 | Release date: | 2014-09-24 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Molecular basis of gain-of-function LEOPARD syndrome-associated SHP2 mutations. Biochemistry, 53, 2014
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4OHL
| LEOPARD Syndrome-Associated SHP2/T468M mutant | Descriptor: | Tyrosine-protein phosphatase non-receptor type 11 | Authors: | Yu, Z.H, Zhang, R.Y, Walls, C.D, Chen, L, Zhang, S, Wu, L, Wang, L, Liu, S, Zhang, Z.Y. | Deposit date: | 2014-01-17 | Release date: | 2014-09-24 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Molecular basis of gain-of-function LEOPARD syndrome-associated SHP2 mutations. Biochemistry, 53, 2014
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7RCT
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4OHH
| LEOPARD Syndrome-Associated SHP2/Q506P mutant | Descriptor: | Tyrosine-protein phosphatase non-receptor type 11 | Authors: | Yu, Z.H, Zhang, R.Y, Walls, C.D, Chen, L, Zhang, S, Wu, L, Wang, L, Liu, S, Zhang, Z.Y. | Deposit date: | 2014-01-17 | Release date: | 2014-09-24 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Molecular basis of gain-of-function LEOPARD syndrome-associated SHP2 mutations. Biochemistry, 53, 2014
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4GWF
| Crystal structure of the tyrosine phosphatase SHP-2 with Y279C mutation | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, GLYCEROL, ... | Authors: | Qiu, W, Lin, A, Hutchinson, A, Romanov, V, Ruzanov, M, Thompson, C, Lam, K, Kisselman, G, Battaile, K, Chirgadze, N.Y. | Deposit date: | 2012-09-03 | Release date: | 2013-09-04 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Crystal structure of the tyrosine phosphatase SHP-2 with Y279C mutation TO BE PUBLISHED
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3HIZ
| Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha | Descriptor: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Authors: | Amzel, L.M, Vogelstein, B, Gabelli, S.B, Mandelker, D. | Deposit date: | 2009-05-20 | Release date: | 2009-09-29 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (3.3 Å) | Cite: | A frequent kinase domain mutation that changes the interaction between PI3K{alpha} and the membrane. Proc.Natl.Acad.Sci.USA, 106, 2009
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7R75
| Structure of human SHP2 in complex with compound 16 | Descriptor: | 6-(4-amino-4-methylpiperidin-1-yl)-3-(3-chlorophenyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, Tyrosine-protein phosphatase non-receptor type 11 | Authors: | Leonard, P.G, Cross, J. | Deposit date: | 2021-06-24 | Release date: | 2021-10-27 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.83 Å) | Cite: | Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor. J.Med.Chem., 64, 2021
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7R7D
| Structure of human SHP2 in complex with compound 22 | Descriptor: | 4-[6-(4-amino-4-methylpiperidin-1-yl)-1H-pyrazolo[3,4-b]pyrazin-3-yl]-3-chloro-N-methylpyridin-2-amine, TETRAETHYLENE GLYCOL, Tyrosine-protein phosphatase non-receptor type 11 | Authors: | Leonard, P.G, Cross, J. | Deposit date: | 2021-06-24 | Release date: | 2021-10-27 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor. J.Med.Chem., 64, 2021
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3HHM
| Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha and the drug wortmannin | Descriptor: | (1S,6BR,9AS,11R,11BR)-9A,11B-DIMETHYL-1-[(METHYLOXY)METHYL]-3,6,9-TRIOXO-1,6,6B,7,8,9,9A,10,11,11B-DECAHYDRO-3H-FURO[4, 3,2-DE]INDENO[4,5-H][2]BENZOPYRAN-11-YL ACETATE, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | Authors: | Amzel, L.M, Vogelstein, B, Gabelli, S.B, Mandelker, D. | Deposit date: | 2009-05-15 | Release date: | 2009-09-29 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | A frequent kinase domain mutation that changes the interaction between PI3K{alpha} and the membrane. Proc.Natl.Acad.Sci.USA, 106, 2009
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7R7L
| Structure of human SHP2 in complex with compound 30 | Descriptor: | 6-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3H)-one, Tyrosine-protein phosphatase non-receptor type 11 | Authors: | Leonard, P.G, Cross, J. | Deposit date: | 2021-06-24 | Release date: | 2021-10-27 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor. J.Med.Chem., 64, 2021
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7R7I
| Structure of human SHP2 in complex with compound 27 | Descriptor: | Tyrosine-protein phosphatase non-receptor type 11, [3-(4-amino-4-methylpiperidin-1-yl)-6-(2,3-dichlorophenyl)-5-methylpyrazin-2-yl]methanol | Authors: | Leonard, P.G, Cross, J. | Deposit date: | 2021-06-24 | Release date: | 2021-10-27 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.85 Å) | Cite: | Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor. J.Med.Chem., 64, 2021
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