7JVM
 
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8ILR
 | | Cryo-EM structure of PI3Kalpha in complex with compound 16 | | Descriptor: | N-[(2S)-1-(ethylamino)-1-oxidanylidene-3-[4-(2-quinoxalin-6-ylethynyl)phenyl]propan-2-yl]-2,3-dimethyl-quinoxaline-6-carboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Zhou, Q, Liu, X, Neri, D, Li, W, Favalli, N, Bassi, G, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | | Deposit date: | 2023-03-04 | | Release date: | 2023-08-30 | | Method: | ELECTRON MICROSCOPY (3.05 Å) | | Cite: | Structural insights into the interaction of three Y-shaped ligands with PI3K alpha.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8ILS
 | | Cryo-EM structure of PI3Kalpha in complex with compound 17 | | Descriptor: | N-[(2R)-1-(ethylamino)-1-oxidanylidene-3-[4-(2-quinoxalin-6-ylethynyl)phenyl]propan-2-yl]-2,3-dimethyl-quinoxaline-6-carboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Zhou, Q, Liu, X, Neri, D, Li, W, Favalli, N, Bassi, G, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | | Deposit date: | 2023-03-04 | | Release date: | 2023-09-13 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structural insights into the interaction of three Y-shaped ligands with PI3K alpha.
Proc.Natl.Acad.Sci.USA, 120, 2023
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4XI2
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4XEY
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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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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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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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6MD9
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6MBZ
 | | Structure of Transcription Factor | | Descriptor: | Signal transducer and activator of transcription 5B | | Authors: | Seo, H.-S, Dhe-Paganon, S. | | Deposit date: | 2018-08-30 | | Release date: | 2019-06-19 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.21 Å) | | Cite: | Structural and functional consequences of the STAT5BN642Hdriver mutation.
Nat Commun, 10, 2019
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6MDA
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8ILV
 | | Cryo-EM structure of PI3Kalpha in complex with compound 18 | | Descriptor: | N-[(2R)-1-(ethylamino)-1-oxidanylidene-3-[3-(2-quinoxalin-6-ylethynyl)phenyl]propan-2-yl]-2,3-dimethyl-quinoxaline-6-carboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Zhou, Q, Liu, X, Neri, D, Li, W, Favalli, N, Bassi, G, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | | Deposit date: | 2023-03-04 | | Release date: | 2023-09-06 | | Method: | ELECTRON MICROSCOPY (3.19 Å) | | Cite: | Structural insights into the interaction of three Y-shaped ligands with PI3K alpha.
Proc.Natl.Acad.Sci.USA, 120, 2023
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5XGJ
 | | Crystal structure of PI3K complex with an inhibitor | | Descriptor: | 3-(4-morpholin-4-ylfuro[3,2-d]pyrimidin-2-yl)-5-[(phenylmethyl)amino]phenol, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | | Authors: | Song, K, Yang, X, Zhao, Y, Jian, Z. | | Deposit date: | 2017-04-13 | | Release date: | 2018-04-25 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (2.97 Å) | | Cite: | Crystal structure of PI3K complex with an inhibitor
To Be Published
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1FMK
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5XGH
 | | Crystal structure of PI3K complex with an inhibitor | | Descriptor: | 3-[(4-fluorophenyl)methylamino]-5-(4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenol, GLYCEROL, Phosphatidylinositol 3-kinase regulatory subunit alpha, ... | | Authors: | Song, K, Yang, X, Zhao, Y, Jian, Z. | | Deposit date: | 2017-04-13 | | Release date: | 2018-04-25 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (2.97 Å) | | Cite: | New Insights into PI3K Inhibitor Design using X-ray Structures of PI3K alpha Complexed with a Potent Lead Compound.
Sci Rep, 7, 2017
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5X7B
 | | Crystal structure of SHP2_SH2-CagA EPIYA_C peptide complex | | Descriptor: | CagA, Tyrosine-protein phosphatase non-receptor type 11 | | Authors: | Senda, M, Senda, T. | | Deposit date: | 2017-02-24 | | Release date: | 2017-09-13 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Differential Mechanisms for SHP2 Binding and Activation Are Exploited by Geographically Distinct Helicobacter pylori CagA Oncoproteins.
Cell Rep, 20, 2017
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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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6E2P
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6E2Q
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4GL9
 | | Crystal structure of inhibitory protein SOCS3 in complex with JAK2 kinase domain and fragment of GP130 intracellular domain | | Descriptor: | 2-TERT-BUTYL-9-FLUORO-3,6-DIHYDRO-7H-BENZ[H]-IMIDAZ[4,5-F]ISOQUINOLINE-7-ONE, Interleukin-6 receptor subunit beta, PHOSPHATE ION, ... | | Authors: | Kershaw, N.J, Murphy, J.M, Laktyushin, A, Nicola, N.A, Babon, J.J. | | Deposit date: | 2012-08-14 | | Release date: | 2013-03-06 | | Last modified: | 2018-06-13 | | Method: | X-RAY DIFFRACTION (3.9 Å) | | Cite: | SOCS3 binds specific receptor-JAK complexes to control cytokine signaling by direct kinase inhibition.
Nat.Struct.Mol.Biol., 20, 2013
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4H34
 | | Crystal structure of the tyrosine phosphatase SHP-2 with Q506P mutation | | Descriptor: | 1,2-ETHANEDIOL, GLYCEROL, Tyrosine-protein phosphatase non-receptor type 11 | | Authors: | Qiu, W, Lin, A, Hutchinson, A, Romanov, V, Ruzanov, M, Thompson, C, Lam, K, Kisselman, G, Battaile, K, Chirgadze, N.Y. | | Deposit date: | 2012-09-13 | | Release date: | 2013-10-02 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Crystal structure of the tyrosine phosphatase SHP-2 with Q506P mutation
To be Published
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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
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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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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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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
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