4XEY
 
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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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4XZ0
 | | ZAP-70-tSH2:compound-A complex | | Descriptor: | 1-(3-{5-[(3-chlorobenzyl)sulfonyl]-1H-tetrazol-1-yl}phenyl)ethanone, SULFATE ION, Tyrosine-protein kinase ZAP-70 | | Authors: | Barros, T, Kuriyan, J, Visperas, P.R, Winger, J.A. | | Deposit date: | 2015-02-03 | | Release date: | 2015-06-17 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2 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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4QSY
 | | SHP2 SH2 domain in complex with GAB1 peptide | | Descriptor: | GRB2-associated-binding protein 1, Tyrosine-protein phosphatase non-receptor type 11 | | Authors: | Gogl, G, Remenyi, A. | | Deposit date: | 2014-07-06 | | Release date: | 2015-07-08 | | Last modified: | 2023-12-06 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Selective targeting of GAB adapter protein SHP2 tyrosine phosphatase interaction attenuates ERK signaling
To be Published
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5BO4
 | | Structure of SOCS2:Elongin C:Elongin B from DMSO-treated crystals | | Descriptor: | Suppressor of cytokine signaling 2, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2 | | Authors: | Gadd, M.S, Bulatov, E, Ciulli, A. | | Deposit date: | 2015-05-27 | | Release date: | 2015-07-08 | | Last modified: | 2017-10-18 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Serendipitous SAD Solution for DMSO-Soaked SOCS2-ElonginC-ElonginB Crystals Using Covalently Incorporated Dimethylarsenic: Insights into Substrate Receptor Conformational Flexibility in Cullin RING Ligases.
Plos One, 10, 2015
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2MRK
 | | Fyn SH2 domain in complex with the natural inhibitory phosphotyrosine peptide | | Descriptor: | C-terminal Tyrosine-protein kinase Fyn, Tyrosine-protein kinase Fyn | | Authors: | Huculeci, R, Buts, L, Lenaerts, A.J, van Nuland, N. | | Deposit date: | 2014-07-09 | | Release date: | 2015-07-15 | | Last modified: | 2016-12-14 | | Method: | SOLUTION NMR | | Cite: | Dynamically Coupled Residues within the SH2 Domain of FYN Are Key to Unlocking Its Activity.
Structure, 24, 2016
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2MRJ
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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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4U1P
 | | Human Fyn-SH2 domain in complex with a synthetic high-affinity phospho-peptide | | Descriptor: | Middle T antigen, POLYETHYLENE GLYCOL (N=34), SODIUM ION, ... | | Authors: | Garcia-Pino, A, Huculeci, R, Lenaerts, T, van Nuland, N.A.J. | | Deposit date: | 2014-07-16 | | Release date: | 2015-07-29 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | Human Fyn-SH2 domain in complex with a synthetic high-affinity phospho-peptide
To Be Published
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4U17
 | | Swapped dimer of the human Fyn-SH2 domain | | Descriptor: | 1,2-ETHANEDIOL, PHOSPHATE ION, Tyrosine-protein kinase Fyn | | Authors: | Garcia-Pino, A, Huculeci, R, Lenaerts, T, van Nuland, N.A.J. | | Deposit date: | 2014-07-15 | | Release date: | 2015-07-29 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.99 Å) | | Cite: | Swapped dimer of the human Fyn-SH2 domain
To Be Published
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2MQI
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4WWQ
 | | Apo structure of the Grb7 SH2 domain | | Descriptor: | Growth factor receptor-bound protein 7, MALONIC ACID | | Authors: | Watson, G.M, Ambaye, N.D, Wilce, M.C, Wilce, J.A. | | Deposit date: | 2014-11-12 | | Release date: | 2015-09-23 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Cyclic Peptides Incorporating Phosphotyrosine Mimetics as Potent and Specific Inhibitors of the Grb7 Breast Cancer Target.
J.Med.Chem., 58, 2015
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4X6S
 | | Grb7 SH2 domain with phosphotyrosine mimetic inhibitor peptide | | Descriptor: | Growth factor receptor-bound protein 7, Phosphotyrosine mimetic inhibitor peptide G7-TEM1 | | Authors: | Watson, G.M, Panjikar, S, Wilce, M.C, Wilce, J.A. | | Deposit date: | 2014-12-09 | | Release date: | 2015-09-23 | | Last modified: | 2015-10-28 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Cyclic Peptides Incorporating Phosphotyrosine Mimetics as Potent and Specific Inhibitors of the Grb7 Breast Cancer Target.
J.Med.Chem., 58, 2015
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5DF6
 | | Crystal structure of PTPN11 tandem SH2 domains in complex with a TXNIP peptide | | Descriptor: | Tyrosine-protein phosphatase non-receptor type 11, UNKNOWN ATOM OR ION, txnip | | Authors: | Dong, A, Li, W, Tempel, W, Liu, Y, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Min, J, Structural Genomics Consortium (SGC) | | Deposit date: | 2015-08-26 | | Release date: | 2015-09-23 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (1.78 Å) | | Cite: | Structural basis for the regulatory role of the PPxY motifs in the thioredoxin-interacting protein TXNIP.
Biochem.J., 473, 2016
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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) | | Descriptor: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, Fibroblast growth factor receptor 2, MAGNESIUM ION, ... | | Authors: | Huang, Z, Li, X, Mohammadi, M. | | Deposit date: | 2015-10-26 | | Release date: | 2016-02-03 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.606 Å) | | Cite: | Two FGF Receptor Kinase Molecules Act in Concert to Recruit and Transphosphorylate Phospholipase C gamma.
Mol.Cell, 61, 2016
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5FI4
 | | Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model | | Descriptor: | GLYCEROL, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | | Authors: | Elling, R.A, Knapp, M.S, Han, W, Daniel, L.M, Xy, Y, Burger, M.T, Ni, Z, Smith, A, Lan, J, Williams, T, Verhagen, J, Huh, K, Merritt, H, Chan, J, Kaufman, S, Voliva, C.F, Pecchi, S. | | Deposit date: | 2015-12-22 | | Release date: | 2016-02-03 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.
Bioorg.Med.Chem.Lett., 26, 2016
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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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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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5DC4
 | | CRYSTAL STRUCTURE OF MONOBODY AS25/ABL1 SH2 DOMAIN COMPLEX, CRYSTAL A | | Descriptor: | AS25 monobody, GLYCEROL, Tyrosine-protein kinase ABL1 | | 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 (1.48 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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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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5I6V
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5IBM
 | | Structure of S502P, 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 (2.18 Å) | | Cite: | Structural and Functional Consequences of Three Cancer-Associated Mutations of the Oncogenic Phosphatase SHP2.
Biochemistry, 55, 2016
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4ZOP
 | | Co-crystal Structure of Lipid Kinase PI3K alpha with a selective phosphatidylinositol-3 kinase alpha inhibitor | | Descriptor: | (2S,3R)-N~1~-(8-tert-butyl-4,5-dihydro[1,3]thiazolo[4,5-h]quinazolin-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide, 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: | 2015-05-06 | | Release date: | 2016-05-18 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.62 Å) | | Cite: | Co-crystal Structure of the Lipid Kinase PI3K alpha with a selective phosphatidylinositol-3 kinase alpha inhibitorCo-crystal Structure of the Lipid Kinase PI3K alpha with a selective phosphatidylinositol-3 kinase alpha inhibitor
To Be Published
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