1M27
 
 | | Crystal structure of SAP/FynSH3/SLAM ternary complex | | 分子名称: | CITRATE ANION, Proto-oncogene tyrosine-protein kinase FYN, SH2 domain protein 1A, ... | | 著者 | Chan, B, Griesbach, J, Song, H.K, Poy, F, Terhorst, C, Eck, M.J. | | 登録日 | 2002-06-21 | | 公開日 | 2003-05-06 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | SAP couples Fyn to SLAM immune receptors.
NAT.CELL BIOL., 5, 2003
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2FO0
 | | Organization of the SH3-SH2 Unit in Active and Inactive Forms of the c-Abl Tyrosine Kinase | | 分子名称: | 6-(2,6-DICHLOROPHENYL)-2-{[3-(HYDROXYMETHYL)PHENYL]AMINO}-8-METHYLPYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE, GLYCEROL, MYRISTIC ACID, ... | | 著者 | Nagar, B, Hantschel, O, Seeliger, M, Davies, J.M, Weis, W.I, Superti-Furga, G, Kuriyan, J. | | 登録日 | 2006-01-12 | | 公開日 | 2006-03-21 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.27 Å) | | 主引用文献 | Organization of the SH3-SH2 unit in active and inactive forms of the c-Abl tyrosine kinase.
Mol.Cell, 21, 2006
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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 | | 分子名称: | CHLORIDE ION, Proto-oncogene tyrosine-protein kinase Fes/Fps, STAUROSPORINE, ... | | 著者 | 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) | | 登録日 | 2008-02-26 | | 公開日 | 2008-03-25 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (1.98 Å) | | 主引用文献 | Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
Cell(Cambridge,Mass.), 134, 2008
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3CBL
 | | Crystal structure of human feline sarcoma viral oncogene homologue (v-FES) in complex with staurosporine and a consensus peptide | | 分子名称: | Proto-oncogene tyrosine-protein kinase Fes/Fps, STAUROSPORINE, Synthetic peptide | | 著者 | 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) | | 登録日 | 2008-02-22 | | 公開日 | 2008-03-04 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
Cell(Cambridge,Mass.), 134, 2008
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4A55
 | | Crystal structure of p110alpha in complex with iSH2 of p85alpha and the inhibitor PIK-108 | | 分子名称: | PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY SUBUNIT ALPHA, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT ALPHA ISOFORM, PIK-108 | | 著者 | Hon, W.-C, Berndt, A, Williams, R.L. | | 登録日 | 2011-10-24 | | 公開日 | 2011-12-28 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (3.5 Å) | | 主引用文献 | Regulation of Lipid Binding Underlies the Activation Mechanism of Class Ia Pi3-Kinases.
Oncogene, 31, 2012
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4D8K
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4DGP
 | | The wild-type Src homology 2 (SH2)-domain containing protein tyrosine phosphatase-2 (SHP2) | | 分子名称: | Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Yu, Z.H, Xu, J, Walls, C.D, Chen, L, Zhang, S, Wu, L, Wang, L.N, Liu, S.J, Zhang, Z.Y. | | 登録日 | 2012-01-26 | | 公開日 | 2013-03-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Structural and Mechanistic Insights into LEOPARD Syndrome-Associated SHP2 Mutations.
J.Biol.Chem., 288, 2013
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8TS9
 | | Human PI3K p85alpha/p110alpha H1047R bound to compound 1 | | 分子名称: | 5-[3-fluoro-5-(trifluoromethyl)benzamido]-N-methyl-6-(2-methylanilino)pyridine-3-carboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Holliday, M, Tang, Y, Bulku, A, Wilbur, J, Fraser, J. | | 登録日 | 2023-08-11 | | 公開日 | 2023-11-22 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.83 Å) | | 主引用文献 | Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3K alpha Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.
Cancer Discov, 14, 2024
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8TSC
 | | Human PI3K p85alpha/p110alpha H1047R bound to compound 3 | | 分子名称: | (1S)-7-[3-fluoro-5-(trifluoromethyl)benzamido]-N-methyl-1-(2-methylphenyl)-3-oxo-2,3-dihydro-1H-isoindole-5-carboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Holliday, M, Tang, Y, Bulku, A, Wilbur, J, Fraser, J. | | 登録日 | 2023-08-11 | | 公開日 | 2023-11-22 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (3.62 Å) | | 主引用文献 | Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3K alpha Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.
Cancer Discov, 14, 2024
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8U7X
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8U7W
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6PBC
 | | Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations | | 分子名称: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma,1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, SODIUM ION | | 著者 | Hajicek, N, Sondek, J. | | 登録日 | 2019-06-13 | | 公開日 | 2020-01-08 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.46 Å) | | 主引用文献 | Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations.
Elife, 8, 2019
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2Y3A
 | | Crystal structure of p110beta in complex with icSH2 of p85beta and the drug GDC-0941 | | 分子名称: | 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 | | 著者 | Zhang, X, Vadas, O, Perisic, O, Williams, R.L. | | 登録日 | 2010-12-20 | | 公開日 | 2011-03-16 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Structure of Lipid Kinase P110Beta-P85Beta Elucidates an Unusual Sh2-Domain-Mediated Inhibitory Mechanism.
Mol.Cell, 41, 2011
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6QHD
 | | Lysine acetylated and tyrosine phosphorylated STAT3 in a complex with DNA | | 分子名称: | 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 | | 著者 | Arbely, E, Belo, Y, Shahar, A, Zarivach, R. | | 登録日 | 2019-01-16 | | 公開日 | 2019-06-19 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | | 主引用文献 | Unexpected implications of STAT3 acetylation revealed by genetic encoding of acetyl-lysine.
Biochim Biophys Acta Gen Subj, 1863, 2019
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3CWG
 | | Unphosphorylated mouse STAT3 core fragment | | 分子名称: | Signal transducer and activator of transcription 3 | | 著者 | Ren, Z, Mao, X, Mertens, C, Krishnaraj, R, Qin, J, Mandal, P.K, Romanowshi, M.J, McMurray, J.S. | | 登録日 | 2008-04-21 | | 公開日 | 2008-07-01 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (3.05 Å) | | 主引用文献 | Crystal structure of unphosphorylated STAT3 core fragment.
Biochem.Biophys.Res.Commun., 374, 2008
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3CXL
 | | Crystal structure of human chimerin 1 (CHN1) | | 分子名称: | N-chimerin, UNKNOWN ATOM OR ION, ZINC ION | | 著者 | 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) | | 登録日 | 2008-04-24 | | 公開日 | 2008-08-05 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Crystal structure of human chimerin 1 (CHN1).
To be Published
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3BKB
 | | Crystal structure of human Feline Sarcoma Viral Oncogene Homologue (v-FES) | | 分子名称: | 1,2-ETHANEDIOL, Proto-oncogene tyrosine-protein kinase Fes/Fps, STAUROSPORINE, ... | | 著者 | 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) | | 登録日 | 2007-12-06 | | 公開日 | 2007-12-25 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.78 Å) | | 主引用文献 | Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation
Cell(Cambridge,Mass.), 134, 2008
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5EHR
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5EHP
 | | Non-receptor Protein Tyrosine Phosphatase SHP2 in Complex with Allosteric Inhibitor SHP836 | | 分子名称: | 5-[2,3-bis(chloranyl)phenyl]-2-[(3~{R},5~{S})-3,5-dimethylpiperazin-1-yl]pyrimidin-4-amine, PHOSPHATE ION, Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Stams, T, Fodor, M. | | 登録日 | 2015-10-28 | | 公開日 | 2016-07-06 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor.
J.Med.Chem., 59, 2016
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5M6U
 | | HUMAN PI3KDELTA IN COMPLEX WITH LASW1579 | | 分子名称: | 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 | | 著者 | Segarra, V, Hernandez, B, Lozoya, E, Blaesse, M, Hoeppner, S, Jestel, A. | | 登録日 | 2016-10-26 | | 公開日 | 2017-02-01 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | | 主引用文献 | 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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5EG3
 | | Crystal Structure of the Activated FGF Receptor 2 (FGFR2) Kinase Domain in complex with the cSH2 domain of Phospholipase C gamma (PLCgamma) | | 分子名称: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, Fibroblast growth factor receptor 2, MAGNESIUM ION, ... | | 著者 | Huang, Z, Li, X, Mohammadi, M. | | 登録日 | 2015-10-26 | | 公開日 | 2016-02-03 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.606 Å) | | 主引用文献 | Two FGF Receptor Kinase Molecules Act in Concert to Recruit and Transphosphorylate Phospholipase C gamma.
Mol.Cell, 61, 2016
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5MO4
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6F3F
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6TLC
 | | Unphosphorylated human STAT3 in complex with MS3-6 monobody | | 分子名称: | Monobody, Signal transducer and activator of transcription 3 | | 著者 | La Sala, G, Lau, K, Reynaud, A, Pojer, F, Hantschel, O. | | 登録日 | 2019-12-02 | | 公開日 | 2020-07-22 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Selective inhibition of STAT3 signaling using monobodies targeting the coiled-coil and N-terminal domains.
Nat Commun, 11, 2020
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5IBS
 | | Structure of E76Q, a Cancer-Associated Mutation of the Oncogenic Phosphatase SHP2 | | 分子名称: | Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Blacklow, S.C, Stams, T, Fodor, M, LaRochelle, J.R. | | 登録日 | 2016-02-22 | | 公開日 | 2016-04-13 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.32 Å) | | 主引用文献 | Structural and Functional Consequences of Three Cancer-Associated Mutations of the Oncogenic Phosphatase SHP2.
Biochemistry, 55, 2016
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