2LQN
 
 | | Solution structure of CRKL | | Descriptor: | Crk-like protein | | Authors: | Jankowski, W, Saleh, T, Kalodimos, C. | | Deposit date: | 2012-03-09 | | Release date: | 2012-05-16 | | Last modified: | 2024-05-15 | | Method: | SOLUTION NMR | | Cite: | Domain organization differences explain Bcr-Abl's preference for CrkL over CrkII.
Nat.Chem.Biol., 8, 2012
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2LQW
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2ABL
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2B3O
 | | Crystal structure of human tyrosine phosphatase SHP-1 | | Descriptor: | Tyrosine-protein phosphatase, non-receptor type 6 | | Authors: | Yang, J, Liu, L, He, D, Song, X, Liang, X, Zhao, Z.J, Zhou, G.W. | | Deposit date: | 2005-09-20 | | Release date: | 2005-10-25 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal structure of human protein-tyrosine phosphatase SHP-1.
J.Biol.Chem., 278, 2003
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2C0I
 | | Src family kinase Hck with bound inhibitor A-420983 | | Descriptor: | CALCIUM ION, N-(4-{4-AMINO-1-[4-(4-METHYLPIPERAZIN-1-YL)-TRANS-CYCLOHEXYL]-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL}-2-METHOXYPHENYL)-1-METHYL-1H-INDOLE-2-CARBOXAMIDE, TYROSINE-PROTEIN KINASE HCK | | Authors: | Borhani, D.W, Burchat, A, Calderwood, D.J, Hirst, G.C, Li, B, Loew, A. | | Deposit date: | 2005-09-03 | | Release date: | 2006-09-20 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of A-770041, a Src-Family Selective Orally Active Lck Inhibitor that Prevents Organ Allograft Rejection.
Bioorg.Med.Chem.Lett., 16, 2006
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2C0T
 | | Src family kinase Hck with bound inhibitor A-641359 | | Descriptor: | CALCIUM ION, N-(4-{4-AMINO-1-[1-(TETRAHYDRO-2H-PYRAN-4-YL)PIPERIDIN-4-YL]-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL}-2-METHOXYPHENYL)-1-METHYL-1H-INDOLE-2-CARBOXAMIDE, TYROSINE-PROTEIN KINASE HCK | | Authors: | Borhani, D.W, Burchat, A, Calderwood, D.J, Hirst, G.C, Li, B, Loew, A. | | Deposit date: | 2005-09-07 | | Release date: | 2006-09-20 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Discovery of A-770041, a Src-Family Selective Orally Active Lck Inhibitor that Prevents Organ Allograft Rejection.
Bioorg.Med.Chem.Lett., 16, 2006
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2C0O
 | | Src family kinase Hck with bound inhibitor A-770041 | | Descriptor: | CALCIUM ION, N-(4-{1-[4-(4-ACETYLPIPERAZIN-1-YL)-TRANS-CYCLOHEXYL]-4-AMINO-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL}-2-METHOXYPHENYL)-1-METHYL-1H-INDOLE-2-CARBOXAMIDE, TYROSINE-PROTEIN KINASE HCK | | Authors: | Borhani, D.W, Burchat, A, Calderwood, D.J, Hirst, G.C, Li, B, Loew, A. | | Deposit date: | 2005-09-06 | | Release date: | 2006-09-20 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | Discovery of A-770041, a Src-Family Selective Orally Active Lck Inhibitor that Prevents Organ Allograft Rejection.
Bioorg.Med.Chem.Lett., 16, 2006
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2C9W
 | | CRYSTAL STRUCTURE OF SOCS-2 IN COMPLEX WITH ELONGIN-B AND ELONGIN-C AT 1.9A RESOLUTION | | Descriptor: | NICKEL (II) ION, SULFATE ION, SUPPRESSOR OF CYTOKINE SIGNALING 2, ... | | Authors: | Debreczeni, J.E, Bullock, A, Amos, A, Savitsky, P, Barr, A, Burgess, N, Sundstrom, M, Weigelt, J, Arrowsmith, C, Edwards, A, Knapp, S. | | Deposit date: | 2005-12-14 | | Release date: | 2006-02-22 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Crystal structure of the SOCS2-elongin C-elongin B complex defines a prototypical SOCS box ubiquitin ligase.
Proc. Natl. Acad. Sci. U.S.A., 103, 2006
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2DVJ
 | | phosphorylated Crk-II | | Descriptor: | V-crk sarcoma virus CT10 oncogene homolog, isoform a | | Authors: | Kobashigawa, Y, Inagaki, F. | | Deposit date: | 2006-07-31 | | Release date: | 2007-05-08 | | 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
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2EYZ
 | | CT10-Regulated Kinase isoform II | | 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: | 2024-05-29 | | Method: | SOLUTION NMR | | Cite: | Structural basis for the transforming activity of human cancer-related signaling adaptor protein CRK.
Nat.Struct.Mol.Biol., 14, 2007
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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: | 2024-05-29 | | Method: | SOLUTION NMR | | Cite: | Structural basis for the transforming activity of human cancer-related signaling adaptor protein CRK.
Nat.Struct.Mol.Biol., 14, 2007
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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
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1OPK
 | | Structural basis for the auto-inhibition of 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, Young, M.A, Scheffzek, K, Veach, D, Bornmann, W, Clarkson, B, Superti-Furga, G, Kuriyan, J. | | Deposit date: | 2003-03-06 | | Release date: | 2003-04-08 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structural basis for the autoinhibition of c-Abl tyrosine kinase
Cell(Cambridge,Mass.), 112, 2003
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1OPL
 | | Structural basis for the auto-inhibition of c-Abl tyrosine kinase | | Descriptor: | 6-(2,6-DICHLOROPHENYL)-2-{[3-(HYDROXYMETHYL)PHENYL]AMINO}-8-METHYLPYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE, MYRISTIC ACID, proto-oncogene tyrosine-protein kinase | | Authors: | Nagar, B, Hantschel, O, Young, M.A, Scheffzek, K, Veach, D, Bornmann, W, Clarkson, B, Superti-Furga, G, Kuriyan, J. | | Deposit date: | 2003-03-06 | | Release date: | 2003-04-08 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (3.42 Å) | | Cite: | Structural basis for the autoinhibition of c-Abl tyrosine kinase
Cell(Cambridge,Mass.), 112, 2003
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1QCF
 | | CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR | | Descriptor: | 1-TER-BUTYL-3-P-TOLYL-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE, Tyrosine-protein kinase HCK | | Authors: | Schindler, T, Sicheri, F, Pico, A, Gazit, A, Levitzki, A, Kuriyan, J. | | Deposit date: | 1999-05-04 | | Release date: | 1999-06-08 | | Last modified: | 2022-12-21 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor.
Mol.Cell, 3, 1999
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1RQQ
 | | Crystal Structure of the Insulin Receptor Kinase in Complex with the SH2 Domain of APS | | Descriptor: | BISUBSTRATE INHIBITOR, Insulin receptor, MANGANESE (II) ION, ... | | Authors: | Hu, J, Liu, J, Ghirlando, R, Saltiel, A.R, Hubbard, S.R. | | Deposit date: | 2003-12-06 | | Release date: | 2003-12-30 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structural basis for recruitment of the adaptor protein APS to the activated insulin receptor.
Mol.Cell, 12, 2003
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1TCE
 | | SOLUTION NMR STRUCTURE OF THE SHC SH2 DOMAIN COMPLEXED WITH A TYROSINE-PHOSPHORYLATED PEPTIDE FROM THE T-CELL RECEPTOR, MINIMIZED AVERAGE STRUCTURE | | Descriptor: | PHOSPHOPEPTIDE OF THE ZETA CHAIN OF T CELL RECEPTOR, SHC | | Authors: | Zhou, M.-M, Meadows, R.P, Logan, T.M, Yoon, H.S, Wade, W.R, Ravichandran, K.S, Burakoff, S.J, Feisk, S.W. | | Deposit date: | 1996-03-27 | | Release date: | 1997-05-15 | | Last modified: | 2022-03-02 | | Method: | SOLUTION NMR | | Cite: | Solution structure of the Shc SH2 domain complexed with a tyrosine-phosphorylated peptide from the T-cell receptor.
Proc.Natl.Acad.Sci.USA, 92, 1995
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1JU5
 | | Ternary complex of an Crk SH2 domain, Crk-derived phophopeptide, and Abl SH3 domain by NMR spectroscopy | | Descriptor: | Abl, Crk | | Authors: | Donaldson, L.W, Pawson, T, Kay, L.E, Forman-Kay, J.D. | | Deposit date: | 2001-08-23 | | Release date: | 2002-11-06 | | Last modified: | 2021-11-10 | | Method: | SOLUTION NMR | | Cite: | Structure of a regulatory complex involving the Abl SH3 domain, the Crk
SH2 domain, and a Crk-derived phosphopeptide
Proc.Natl.Acad.Sci.USA, 99, 2002
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1K9A
 | | Crystal structure analysis of full-length carboxyl-terminal Src kinase at 2.5 A resolution | | Descriptor: | Carboxyl-terminal Src kinase | | Authors: | Ogawa, A, Takayama, Y, Nagata, A, Chong, K.T, Takeuchi, S, Sakai, H, Nakagawa, A, Nada, S, Okada, M, Tsukihara, T. | | Deposit date: | 2001-10-28 | | Release date: | 2002-03-20 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structure of the carboxyl-terminal Src kinase, Csk.
J.Biol.Chem., 277, 2002
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1KSW
 | | Structure of Human c-Src Tyrosine Kinase (Thr338Gly Mutant) in Complex with N6-benzyl ADP | | Descriptor: | N6-BENZYL ADENOSINE-5'-DIPHOSPHATE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Witucki, L.A, Huang, X, Shah, K, Liu, Y, Kyin, S, Eck, M.J, Shokat, K.M. | | Deposit date: | 2002-01-14 | | Release date: | 2002-02-27 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Mutant tyrosine kinases with unnatural nucleotide specificity retain the structure and phospho-acceptor specificity of the wild-type enzyme.
Chem.Biol., 9, 2002
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1LCK
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1M27
 | | Crystal structure of SAP/FynSH3/SLAM ternary complex | | Descriptor: | CITRATE ANION, Proto-oncogene tyrosine-protein kinase FYN, SH2 domain protein 1A, ... | | Authors: | Chan, B, Griesbach, J, Song, H.K, Poy, F, Terhorst, C, Eck, M.J. | | Deposit date: | 2002-06-21 | | Release date: | 2003-05-06 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | SAP couples Fyn to SLAM immune receptors.
NAT.CELL BIOL., 5, 2003
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8V8H
 | | PI3Ka H1047R co-crystal structure with inhibitor in cryptic pocket near H1047R (compound 4). | | Descriptor: | (2S)-N~1~-[(4P)-2-tert-butyl-4'-methyl[4,5'-bi-1,3-thiazol]-2'-yl]pyrrolidine-1,2-dicarboxamide, 2-({(1R)-1-[2-(4,4-dimethylpiperidin-1-yl)-3,6-dimethyl-4-oxo-4H-1-benzopyran-8-yl]ethyl}amino)benzoic acid, Phosphatidylinositol 3-kinase regulatory subunit alpha, ... | | Authors: | Gunn, R.J, Lawson, J.D. | | Deposit date: | 2023-12-05 | | Release date: | 2024-03-20 | | Last modified: | 2024-04-10 | | Method: | X-RAY DIFFRACTION (3.58 Å) | | Cite: | Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3K alpha Mutant Protein.
J.Med.Chem., 67, 2024
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8T7Q
 | | Identification of GDC-1971 (RLY-1971), a SHP2 inhibitor designed for the treatment of solid tumors | | Descriptor: | 1-{3-[(2-chlorophenyl)sulfanyl]-1H-pyrazolo[3,4-b]pyrazin-6-yl}-4-methylpiperidin-4-amine, Tyrosine-protein phosphatase non-receptor type 11 | | Authors: | Tang, Y, Nguyen, V, Wilbur, J.D. | | Deposit date: | 2023-06-21 | | Release date: | 2023-10-11 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors.
J.Med.Chem., 66, 2023
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8W9A
 | | CryoEM structure of human PI3K-alpha (P85/P110-H1047R) with QR-7909 binding at an allosteric site | | Descriptor: | 6-chloranyl-3-[[(1R)-1-[2-(1,3-dihydropyrrolo[3,4-c]pyridin-2-yl)-3,6-dimethyl-4-oxidanylidene-quinazolin-8-yl]ethyl]amino]pyridine-2-carboxylic acid, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Huang, X, Ren, X, Zhong, W. | | Deposit date: | 2023-09-05 | | Release date: | 2024-04-17 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | Cryo-EM structures reveal two allosteric inhibition modes of PI3K alpha H1047R involving a re-shaping of the activation loop.
Structure, 2024
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