4FL2
 
 | | Structural and Biophysical Characterization of the Syk Activation Switch | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Tyrosine-protein kinase SYK | | Authors: | Graedler, U, Schwarz, D, Dresing, V, Musil, M, Bomke, J, Frech, M, Jaekel, S, Rysiok, T, Mueller-Pompalla, D, Wegener, A. | | Deposit date: | 2012-06-14 | | Release date: | 2012-11-28 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.19 Å) | | Cite: | Structural and biophysical characterization of the syk activation switch.
J.Mol.Biol., 425, 2013
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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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4OHE
 | | LEOPARD Syndrome-Associated SHP2/G464A 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 (2.506 Å) | | Cite: | Molecular basis of gain-of-function LEOPARD syndrome-associated SHP2 mutations.
Biochemistry, 53, 2014
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5DC0
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5DC9
 | | CRYSTAL STRUCTURE OF MONOBODY AS25/ABL1 SH2 DOMAIN COMPLEX, CRYSTAL B | | Descriptor: | AS25 monobody, GLYCEROL, IMIDAZOLE, ... | | Authors: | Wojcik, J.B, Koide, A, Koide, S. | | Deposit date: | 2015-08-23 | | Release date: | 2016-03-02 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (1.56 Å) | | Cite: | Allosteric Inhibition of Bcr-Abl Kinase by High Affinity Monobody Inhibitors Directed to the Src Homology 2 (SH2)-Kinase Interface.
J.Biol.Chem., 291, 2016
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4OVU
 | | Crystal Structure of p110alpha in complex with niSH2 of p85alpha | | Descriptor: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Gabelli, S.B, Vogelstein, B, Miller, M.S, Amzel, L.M. | | Deposit date: | 2014-01-14 | | Release date: | 2014-09-03 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.96 Å) | | Cite: | Structural basis of nSH2 regulation and lipid binding in PI3K alpha.
Oncotarget, 5, 2014
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4OVV
 | | Crystal Structure of PI3Kalpha in complex with diC4-PIP2 | | Descriptor: | (2R)-3-{[(R)-HYDROXY{[(1R,2R,3S,4R,5R,6S)-2,3,6-TRIHYDROXY-4,5-BIS(PHOSPHONOOXY)CYCLOHEXYL]OXY}PHOSPHORYL]OXY}PROPANE-1 ,2-DIYL DIBUTANOATE, PHOSPHATE ION, Phosphatidylinositol 3-kinase regulatory subunit alpha, ... | | Authors: | Gabelli, S.B, Vogelstein, B, Miller, M, Amzel, L.M. | | Deposit date: | 2014-01-14 | | Release date: | 2014-09-03 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Structural basis of nSH2 regulation and lipid binding in PI3K alpha.
Oncotarget, 5, 2014
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4OHD
 | | LEOPARD Syndrome-Associated SHP2/A461T 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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4U5W
 | | Crystal Structure of HIV-1 Nef-SF2 Core Domain in Complex with the Src Family Kinase Hck SH3-SH2 Tandem Regulatory Domains | | Descriptor: | (4S)-2-METHYL-2,4-PENTANEDIOL, IODIDE ION, Protein Nef, ... | | Authors: | Alvarado, J.J, Yeh, J.I, Smithgall, T.E. | | Deposit date: | 2014-07-25 | | Release date: | 2014-08-20 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.86 Å) | | Cite: | Interaction with the Src Homology (SH3-SH2) Region of the Src-family Kinase Hck Structures the HIV-1 Nef Dimer for Kinase Activation and Effector Recruitment.
J.Biol.Chem., 289, 2014
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4WAF
 | | Crystal Structure of a novel tetrahydropyrazolo[1,5-a]pyrazine in an engineered PI3K alpha | | Descriptor: | N,N-dimethyl-4-[(6R)-6-methyl-5-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl]benzenesulfonamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Knapp, M.S, Elling, R.A. | | Deposit date: | 2014-08-29 | | Release date: | 2014-12-31 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.39 Å) | | Cite: | Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.
Acs Med.Chem.Lett., 6, 2015
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6PBC
 | | Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations | | Descriptor: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma,1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, SODIUM ION | | Authors: | Hajicek, N, Sondek, J. | | Deposit date: | 2019-06-13 | | Release date: | 2020-01-08 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.46 Å) | | Cite: | Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations.
Elife, 8, 2019
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6QHD
 | | Lysine acetylated and tyrosine phosphorylated STAT3 in a complex with DNA | | Descriptor: | DNA (5'-D(*AP*AP*GP*AP*TP*TP*TP*AP*CP*GP*GP*GP*AP*AP*AP*TP*GP*C)-3'), DNA (5'-D(*TP*GP*CP*AP*TP*TP*TP*CP*CP*CP*GP*TP*AP*AP*AP*TP*CP*T)-3'), Signal transducer and activator of transcription 3 | | Authors: | Arbely, E, Belo, Y, Shahar, A, Zarivach, R. | | Deposit date: | 2019-01-16 | | Release date: | 2019-06-19 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | Unexpected implications of STAT3 acetylation revealed by genetic encoding of acetyl-lysine.
Biochim Biophys Acta Gen Subj, 1863, 2019
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5M6U
 | | HUMAN PI3KDELTA IN COMPLEX WITH LASW1579 | | Descriptor: | 4-azanyl-6-[[(1~{S})-1-(4-oxidanylidene-3-phenyl-pyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl]amino]pyrimidine-5-carbonitrile, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | | Authors: | Segarra, V, Hernandez, B, Lozoya, E, Blaesse, M, Hoeppner, S, Jestel, A. | | Deposit date: | 2016-10-26 | | Release date: | 2017-02-01 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | Discovery of a Potent, Selective, and Orally Available PI3K delta Inhibitor for the Treatment of Inflammatory Diseases.
ACS Med Chem Lett, 8, 2017
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3CWG
 | | Unphosphorylated mouse STAT3 core fragment | | Descriptor: | Signal transducer and activator of transcription 3 | | Authors: | Ren, Z, Mao, X, Mertens, C, Krishnaraj, R, Qin, J, Mandal, P.K, Romanowshi, M.J, McMurray, J.S. | | Deposit date: | 2008-04-21 | | Release date: | 2008-07-01 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (3.05 Å) | | Cite: | Crystal structure of unphosphorylated STAT3 core fragment.
Biochem.Biophys.Res.Commun., 374, 2008
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6F3F
 | | Autoinhibited Src kinase bound to ADP | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Tyrosine-protein kinase | | Authors: | von Raussendorf, F, Leonard, T.A. | | Deposit date: | 2017-11-28 | | Release date: | 2017-12-27 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.41795778 Å) | | Cite: | A switch in nucleotide affinity governs activation of the Src and Tec family kinases.
Sci Rep, 7, 2017
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5MO4
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3BKB
 | | Crystal structure of human Feline Sarcoma Viral Oncogene Homologue (v-FES) | | Descriptor: | 1,2-ETHANEDIOL, Proto-oncogene tyrosine-protein kinase Fes/Fps, STAUROSPORINE, ... | | Authors: | Filippakopoulos, P, Salah, E, Fedorov, O, Cooper, C, Ugochukwu, E, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2007-12-06 | | Release date: | 2007-12-25 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.78 Å) | | Cite: | Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
Cell(Cambridge,Mass.), 134, 2008
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3CXL
 | | Crystal structure of human chimerin 1 (CHN1) | | Descriptor: | N-chimerin, UNKNOWN ATOM OR ION, ZINC ION | | Authors: | Shen, L, Buck, M, Tong, Y, Tempel, W, MacKenzie, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Wilkstrom, M, Bochkarev, A, Park, H, Structural Genomics Consortium (SGC) | | Deposit date: | 2008-04-24 | | Release date: | 2008-08-05 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Crystal structure of human chimerin 1 (CHN1).
To be Published
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3CD3
 | | Crystal structure of phosphorylated human feline sarcoma viral oncogene homologue (v-FES) in complex with staurosporine and a consensus peptide | | Descriptor: | CHLORIDE ION, Proto-oncogene tyrosine-protein kinase Fes/Fps, STAUROSPORINE, ... | | Authors: | Filippakopoulos, P, Salah, E, Cooper, C, Picaud, S.S, Elkins, J.M, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2008-02-26 | | Release date: | 2008-03-25 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (1.98 Å) | | Cite: | Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
Cell(Cambridge,Mass.), 134, 2008
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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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3CBL
 | | Crystal structure of human feline sarcoma viral oncogene homologue (v-FES) in complex with staurosporine and a consensus peptide | | Descriptor: | Proto-oncogene tyrosine-protein kinase Fes/Fps, STAUROSPORINE, Synthetic peptide | | Authors: | Filippakopoulos, P, Salah, E, Cooper, C, Picaud, S.S, Elkins, J.M, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2008-02-22 | | Release date: | 2008-03-04 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
Cell(Cambridge,Mass.), 134, 2008
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5IBS
 | | Structure of E76Q, a Cancer-Associated Mutation of the Oncogenic Phosphatase SHP2 | | Descriptor: | Tyrosine-protein phosphatase non-receptor type 11 | | Authors: | Blacklow, S.C, Stams, T, Fodor, M, LaRochelle, J.R. | | Deposit date: | 2016-02-22 | | Release date: | 2016-04-13 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.32 Å) | | Cite: | Structural and Functional Consequences of Three Cancer-Associated Mutations of the Oncogenic Phosphatase SHP2.
Biochemistry, 55, 2016
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7Q5T
 | | The tandem SH2 domains of SYK with a bound FCER1G diphospho-ITAM peptide | | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, High affinity immunoglobulin epsilon receptor subunit gamma, ... | | Authors: | Bradshaw, W.J, Katis, V.L, Chen, Z, Bountra, C, von Delft, F, Gileadi, O, Brennan, P.E. | | Deposit date: | 2021-11-04 | | Release date: | 2021-11-24 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | The tandem SH2 domains of SYK
To Be Published
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7Q5U
 | | The tandem SH2 domains of SYK with a bound CD3G diphospho-ITAM peptide | | Descriptor: | 1,2-ETHANEDIOL, 1-ETHOXY-2-(2-ETHOXYETHOXY)ETHANE, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Bradshaw, W.J, Katis, V.L, Chen, Z, Bountra, C, von Delft, F, Gileadi, O, Brennan, P.E. | | Deposit date: | 2021-11-04 | | Release date: | 2021-11-24 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | The tandem SH2 domains of SYK
To Be Published
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5I6V
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