4NWG
| Crystal structure of the tyrosine phosphatase SHP-2 with E139D mutation | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, SULFATE ION, ... | Authors: | Qiu, W, Lin, A, Hutchinson, A, Romanov, V, Ruzanov, M, Thompson, C, Lam, K, Kisselman, G, Battalie, K, Chirgadze, N.Y. | Deposit date: | 2013-12-06 | Release date: | 2014-12-10 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.45 Å) | Cite: | Crystal structure of the tyrosine phosphatase SHP-2 with E139D mutation To be Published
|
|
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
|
|
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
|
|
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
|
|
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
|
|
6TLC
| Unphosphorylated human STAT3 in complex with MS3-6 monobody | Descriptor: | Monobody, Signal transducer and activator of transcription 3 | Authors: | La Sala, G, Lau, K, Reynaud, A, Pojer, F, Hantschel, O. | Deposit date: | 2019-12-02 | Release date: | 2020-07-22 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Selective inhibition of STAT3 signaling using monobodies targeting the coiled-coil and N-terminal domains. Nat Commun, 11, 2020
|
|
5DC0
| |
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
|
|
2EYY
| CT10-Regulated Kinase isoform I | Descriptor: | v-crk sarcoma virus CT10 oncogene homolog isoform a | Authors: | Kobashigawa, Y, Tanaka, S, Inagaki, F. | Deposit date: | 2005-11-10 | Release date: | 2006-11-10 | Last modified: | 2022-03-09 | Method: | SOLUTION NMR | Cite: | Structural basis for the transforming activity of human cancer-related signaling adaptor protein CRK. Nat.Struct.Mol.Biol., 14, 2007
|
|
2FO0
| Organization of the SH3-SH2 Unit in Active and Inactive Forms of the c-Abl Tyrosine Kinase | Descriptor: | 6-(2,6-DICHLOROPHENYL)-2-{[3-(HYDROXYMETHYL)PHENYL]AMINO}-8-METHYLPYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE, GLYCEROL, MYRISTIC ACID, ... | Authors: | Nagar, B, Hantschel, O, Seeliger, M, Davies, J.M, Weis, W.I, Superti-Furga, G, Kuriyan, J. | Deposit date: | 2006-01-12 | Release date: | 2006-03-21 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.27 Å) | Cite: | Organization of the SH3-SH2 unit in active and inactive forms of the c-Abl tyrosine kinase. Mol.Cell, 21, 2006
|
|
2Y3A
| Crystal structure of p110beta in complex with icSH2 of p85beta and the drug GDC-0941 | Descriptor: | 2-(1H-indazol-4-yl)-6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-yl-thieno[3,2-d]pyrimidine, PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY SUBUNIT BETA, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT BETA ISOFORM | Authors: | Zhang, X, Vadas, O, Perisic, O, Williams, R.L. | Deposit date: | 2010-12-20 | Release date: | 2011-03-16 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (3.3 Å) | Cite: | Structure of Lipid Kinase P110Beta-P85Beta Elucidates an Unusual Sh2-Domain-Mediated Inhibitory Mechanism. Mol.Cell, 41, 2011
|
|
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
|
|
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
|
|
6UX2
| Crystal structure of ZIKV RdRp in complex with STAT2 | Descriptor: | Nonstructural Protein 5, SULFATE ION, Signal transducer and activator of transcription 2, ... | Authors: | Wang, B, Song, J. | Deposit date: | 2019-11-06 | Release date: | 2020-07-08 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (3.01 Å) | Cite: | Structural basis for STAT2 suppression by flavivirus NS5. Nat.Struct.Mol.Biol., 27, 2020
|
|
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
|
|
1LCK
| |
4E93
| Crystal structure of human Feline Sarcoma Viral Oncogene Homologue (v-FES)in complex with TAE684 | Descriptor: | 5-CHLORO-N-[2-METHOXY-4-[4-(4-METHYLPIPERAZIN-1-YL)PIPERIDIN-1-YL]PHENYL]-N'-(2-PROPAN-2-YLSULFONYLPHENYL)PYRIMIDINE-2,4-DIAMINE, Tyrosine-protein kinase Fes/Fps | Authors: | Filippakopoulos, P, Salah, E, Miduturu, C.V, Fedorov, O, Cooper, C, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Gray, N.S, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2012-03-20 | Release date: | 2012-04-18 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (1.84 Å) | Cite: | Small-Molecule Inhibitors of the c-Fes Protein-Tyrosine Kinase. Chem.Biol., 19, 2012
|
|
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
|
|
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
|
|
5MO4
| |
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
|
|
4A55
| Crystal structure of p110alpha in complex with iSH2 of p85alpha and the inhibitor PIK-108 | Descriptor: | PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY SUBUNIT ALPHA, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT ALPHA ISOFORM, PIK-108 | Authors: | Hon, W.-C, Berndt, A, Williams, R.L. | Deposit date: | 2011-10-24 | Release date: | 2011-12-28 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (3.5 Å) | Cite: | Regulation of Lipid Binding Underlies the Activation Mechanism of Class Ia Pi3-Kinases. Oncogene, 31, 2012
|
|
7PG5
| Crystal Structure of PI3Kalpha | Descriptor: | GLYCEROL, PHOSPHATE ION, Phosphatidylinositol 3-kinase regulatory subunit alpha, ... | Authors: | Gong, G, Pinotsis, N, Williams, R.L, Vanhaesebroeck, B. | Deposit date: | 2021-08-13 | Release date: | 2022-08-24 | Last modified: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2.20029068 Å) | Cite: | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration. Nature, 618, 2023
|
|
7PG6
| Crystal Structure of PI3Kalpha in complex with the inhibitor NVP-BYL719 | Descriptor: | (2S)-N~1~-{4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl}pyrrolidine-1,2-dicarboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | Authors: | Gong, G, Pinotsis, N, Williams, R.L, Vanhaesebroeck, B. | Deposit date: | 2021-08-13 | Release date: | 2022-08-24 | Last modified: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2.49943733 Å) | Cite: | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration. Nature, 618, 2023
|
|
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
|
|