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
|
|
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
|
|
2B4S
 | | Crystal structure of a complex between PTP1B and the insulin receptor tyrosine kinase | | Descriptor: | Insulin receptor, SULFATE ION, Tyrosine-protein phosphatase, ... | | Authors: | Li, S, Depetris, R.S, Barford, D, Chernoff, J, Hubbard, S.R. | | Deposit date: | 2005-09-26 | | Release date: | 2005-11-15 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Crystal Structure of a Complex between Protein Tyrosine Phosphatase 1B and the Insulin Receptor Tyrosine Kinase.
Structure, 13, 2005
|
|
2B7A
 | | The structural basis of Janus Kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor | | Descriptor: | 2-TERT-BUTYL-9-FLUORO-3,6-DIHYDRO-7H-BENZ[H]-IMIDAZ[4,5-F]ISOQUINOLINE-7-ONE, Tyrosine-protein kinase JAK2 | | Authors: | Lucet, I.S, Fantino, E, Styles, M, Bamert, R, Patel, O, Broughton, S.E, Walter, M, Burns, C.J, Treutlein, H, Wilks, A.F, Rossjohn, J. | | Deposit date: | 2005-10-04 | | Release date: | 2006-01-10 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor.
Blood, 107, 2006
|
|
2BDJ
 | | Src kinase in complex with inhibitor AP23464 | | Descriptor: | 3-[2-(2-CYCLOPENTYL-6-{[4-(DIMETHYLPHOSPHORYL)PHENYL]AMINO}-9H-PURIN-9-YL)ETHYL]PHENOL, Proto-oncogene tyrosine-protein kinase Src | | Authors: | Dalgarno, D, Stehle, T, Schelling, P, Narula, S, Sawyer, T. | | Deposit date: | 2005-10-20 | | Release date: | 2006-10-24 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.
Chem.Biol.Drug Des., 67, 2006
|
|
2BDF
 | | Src kinase in complex with inhibitor AP23451 | | Descriptor: | Proto-oncogene tyrosine-protein kinase Src, {[(4-{[2-(4-AMINOCYCLOHEXYL)-9-ETHYL-9H-PURIN-6-YL]AMINO}PHENYL)(HYDROXY)PHOSPHORYL]METHYL}PHOSPHONIC ACID | | Authors: | Dalgarno, D, Stehle, T, Schelling, P, Sawyer, T, Narula, S. | | Deposit date: | 2005-10-20 | | Release date: | 2006-10-24 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.
Chem.Biol.Drug Des., 67, 2006
|
|
2ETM
 | |
2EVA
 | | Structural Basis for the Interaction of TAK1 Kinase with its Activating Protein TAB1 | | Descriptor: | ADENOSINE, TAK1 kinase - TAB1 chimera fusion protein | | Authors: | Brown, K, Vial, S.C, Dedi, N, Long, J.M, Dunster, N.J, Cheetham, G.M. | | Deposit date: | 2005-10-31 | | Release date: | 2006-05-02 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural basis for the interaction of TAK1 kinase with its activating protein TAB1
J.Mol.Biol., 354, 2005
|
|
2F4J
 | | Structure of the Kinase Domain of an Imatinib-Resistant Abl Mutant in Complex with the Aurora Kinase Inhibitor VX-680 | | Descriptor: | CYCLOPROPANECARBOXYLIC ACID {4-[4-(4-METHYL-PIPERAZIN-1-YL)-6-(5-METHYL-2H-PYRAZOL-3-YLAMINO)-PYRIMIDIN-2-YLSULFANYL]-PHENYL}-AMIDE, Proto-oncogene tyrosine-protein kinase ABL1 | | Authors: | Young, M.A, Shah, N.P, Chao, L.H, Zarrinkar, P, Sawyers, P, Kuriyan, J. | | Deposit date: | 2005-11-23 | | Release date: | 2006-01-24 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.91 Å) | | Cite: | Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.
Cancer Res., 66, 2006
|
|
2FB8
 | | Structure of the B-Raf kinase domain bound to SB-590885 | | Descriptor: | (1Z)-5-(2-{4-[2-(DIMETHYLAMINO)ETHOXY]PHENYL}-5-PYRIDIN-4-YL-1H-IMIDAZOL-4-YL)INDAN-1-ONE OXIME, B-Raf proto-oncogene serine/threonine-protein kinase | | Authors: | Lougheed, J.C, Lee, J, Chau, D.C, Stout, T.J. | | Deposit date: | 2005-12-08 | | Release date: | 2006-12-12 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.
Cancer Res., 66, 2006
|
|
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
|
|
2G15
 | | Structural Characterization of autoinhibited c-Met kinase | | Descriptor: | activated met oncogene | | Authors: | Wang, W, Marimuthu, A, Tsai, J, Kumar, A, Krupka, H.I, Zhang, C, Powell, B, Suzuki, Y, Nguyen, H, Tabrizizad, M, Luu, C, West, B.L. | | Deposit date: | 2006-02-13 | | Release date: | 2006-03-21 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Structural characterization of autoinhibited c-Met kinase produced by coexpression in bacteria with phosphatase.
Proc.Natl.Acad.Sci.Usa, 103, 2006
|
|
2G1T
 | |
2G2F
 | |
2G2H
 | |
2G2I
 | |
2GQG
 | | X-ray Crystal Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain | | Descriptor: | GLYCEROL, N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE, Proto-oncogene tyrosine-protein kinase ABL1 | | Authors: | Klei, H.E. | | Deposit date: | 2006-04-20 | | Release date: | 2006-11-21 | | Last modified: | 2017-10-18 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | The Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain Elucidates Its Inhibitory Activity against Imatinib-Resistant ABL Mutants
CANCER RES., 66, 2006
|
|
2GS6
 | | Crystal Structure of the active EGFR kinase domain in complex with an ATP analog-peptide conjugate | | Descriptor: | CHLORIDE ION, Epidermal growth factor receptor, Peptide, ... | | Authors: | Zhang, X, Gureasko, J, Shen, K, Cole, P.A, Kuriyan, J. | | Deposit date: | 2006-04-25 | | Release date: | 2006-06-20 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | An Allosteric Mechanism for Activation of the Kinase Domain of Epidermal Growth Factor Receptor
Cell(Cambridge,Mass.), 125, 2006
|
|
2GS7
 | | Crystal Structure of the inactive EGFR kinase domain in complex with AMP-PNP | | Descriptor: | Epidermal growth factor receptor, IODIDE ION, MAGNESIUM ION, ... | | Authors: | Zhang, X, Gureasko, J, Shen, K, Cole, P.A, Kuriyan, J. | | Deposit date: | 2006-04-25 | | Release date: | 2006-06-20 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor
Cell(Cambridge,Mass.), 125, 2006
|
|
2GS2
 | | Crystal Structure of the active EGFR kinase domain | | Descriptor: | Epidermal growth factor receptor | | Authors: | Zhang, X, Gureasko, J, Shen, K, Cole, P.A, Kuriyan, J. | | Deposit date: | 2006-04-25 | | Release date: | 2006-06-20 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor.
Cell(Cambridge,Mass.), 125, 2006
|
|
2GSF
 | | The Human Epha3 Receptor Tyrosine Kinase and Juxtamembrane Region | | Descriptor: | Ephrin type-A receptor 3 | | Authors: | Walker, J.R, Davis, T, Dong, A, Newman, E.M, MacKenzie, F, Weigelt, J, Sundstrom, M, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2006-04-26 | | Release date: | 2006-06-13 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.77 Å) | | Cite: | Structure Of The Human Epha3 Receptor Tyrosine Kinase and Juxtamembrane Region
To be Published
|
|
2DQ7
 | |
2ITW
 | | Crystal structure of EGFR kinase domain in complex with AFN941 | | Descriptor: | 1,2,3,4-Tetrahydrogen Staurosporine, EPIDERMAL GROWTH FACTOR RECEPTOR | | Authors: | Yun, C.-H, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | Deposit date: | 2006-05-25 | | Release date: | 2007-04-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.88 Å) | | Cite: | Structures of Lung Cancer-Derived Egfr Mutants and Inhibitor Complexes: Mechanism of Activation and Insights Into Differential Inhibitor Sensitivity
Cancer Cell, 11, 2007
|
|
2ITT
 | | Crystal structure of EGFR kinase domain L858R mutation in complex with AEE788 | | Descriptor: | 6-{4-[(4-ETHYLPIPERAZIN-1-YL)METHYL]PHENYL}-N-[(1R)-1-PHENYLETHYL]-7H-PYRROLO[2,3-D]PYRIMIDIN-4-AMINE, EPIDERMAL GROWTH FACTOR RECEPTOR | | Authors: | Yun, C.-H, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | Deposit date: | 2006-05-25 | | Release date: | 2007-04-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.73 Å) | | Cite: | Structures of Lung Cancer-Derived Egfr Mutants and Inhibitor Complexes: Mechanism of Activation and Insights Into Differential Inhibitor Sensitivity
Cancer Cell, 11, 2007
|
|
2ITV
 | | Crystal structure of EGFR kinase domain L858R mutation in complex with AMP-PNP | | Descriptor: | EPIDERMAL GROWTH FACTOR RECEPTOR, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | Authors: | Yun, C.-H, Boggon, T.J, Li, Y, Woo, S, Greulich, H, Meyerson, M, Eck, M.J. | | Deposit date: | 2006-05-25 | | Release date: | 2007-04-03 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.47 Å) | | Cite: | Structures of Lung Cancer-Derived Egfr Mutants and Inhibitor Complexes: Mechanism of Activation and Insights Into Differential Inhibitor Sensitivity
Cancer Cell, 11, 2007
|
|
