3TZ9
 
 | | Kinase domain of cSrc in complex with RL130 | | 分子名称: | 1-[1-(3-aminophenyl)-3-tert-butyl-1H-pyrazol-5-yl]-3-[4-(quinazolin-4-ylamino)phenyl]urea, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Gruetter, C, Richters, A, Rauh, D. | | 登録日 | 2011-09-27 | | 公開日 | 2012-10-10 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Overcoming Gatekeeper Mutations in cSrc and Abl by Hybrid Compound Design
To be Published
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1MP8
 | | Crystal structure of Focal Adhesion Kinase (FAK) | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, focal adhesion kinase 1 | | 著者 | Nowakowski, J, Cronin, C.N, McRee, D.E, Knuth, M.W, Nelson, C.G, Pavletich, N.P, Rodgers, J, Sang, B.-C, Scheibe, D.N, Swanson, R.V, Thompson, D.A. | | 登録日 | 2002-09-11 | | 公開日 | 2003-09-16 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Structures of the cancer-related Aurora-A, FAK, and EphA2 protein kinases from nanovolume crystallography
Structure, 10, 2002
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1M52
 | | Crystal Structure of the c-Abl Kinase domain in complex with PD173955 | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 6-(2,6-DICHLORO-PHENYL)-8-METHYL-2-(3-METHYLSULFANYL-PHENYLAMINO)-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ABL1 | | 著者 | Nagar, B, Bornmann, W, Pellicena, P, Schindler, T, Veach, D, Miller, W.T, Clarkson, B, Kuriyan, J. | | 登録日 | 2002-07-08 | | 公開日 | 2002-09-18 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Crystal Structures of the Kinase Domain of c-Abl in Complex with the Small Molecule Inhibitors PD173955 and Imatinib (STI-571)
Cancer Res., 62, 2002
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1P14
 | | Crystal structure of a catalytic-loop mutant of the insulin receptor tyrosine kinase | | 分子名称: | insulin receptor | | 著者 | Li, S, Covino, N.D, Stein, E.G, Till, J.H, Hubbard, S.R. | | 登録日 | 2003-04-11 | | 公開日 | 2003-07-22 | | 最終更新日 | 2023-08-16 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Structural and biochemical evidence for an autoinhibitory role for tyrosine 984 in the juxtamembrane region of the insulin receptor
J.Biol.Chem., 278, 2003
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1P4O
 | | Structure of Apo unactivated IGF-1R KInase domain at 1.5A resolution. | | 分子名称: | Insulin-like growth factor I receptor protein | | 著者 | Munshi, S, Kornienko, M, Hall, D.L, Darke, P.L, Waxman, L, Kuo, L.C. | | 登録日 | 2003-04-23 | | 公開日 | 2003-04-29 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 A resolution.
Acta Crystallogr.,Sect.D, 59, 2003
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1OPJ
 | | Structural basis for the auto-inhibition of c-Abl tyrosine kinase | | 分子名称: | 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, CHLORIDE ION, MYRISTIC ACID, ... | | 著者 | Nagar, B, Hantschel, O, Young, M.A, Scheffzek, K, Veach, D, Bornmann, W, Clarkson, B, Superti-Furga, G, Kuriyan, J. | | 登録日 | 2003-03-06 | | 公開日 | 2003-04-08 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Structural basis for the autoinhibition of c-Abl tyrosine kinase
Cell(Cambridge,Mass.), 112, 2003
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1OEC
 | | FGFr2 kinase domain | | 分子名称: | 4-ARYL-2-PHENYLAMINO PYRIMIDINE, FIBROBLAST GROWTH FACTOR RECEPTOR 2, SULFATE ION | | 著者 | Ceska, T.A, Owens, R, Doyle, C, Hamlyn, P, Crabbe, T, Moffat, D, Davis, J, Martin, R, Perry, M.J. | | 登録日 | 2003-03-24 | | 公開日 | 2004-10-27 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | The Crystal Structure of the Fgfr2 Tyrosine Kinase Domain in Complex with 4-Aryl-2-Phenylamino Pyrimidine Angiogenesis Inhibitors
To be Published
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1PKG
 | | Structure of a c-Kit Kinase Product Complex | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, c-kit protein | | 著者 | Mol, C.D, Lim, K.B, Sridhar, V, Zou, H, Chien, E.Y.T, Sang, B.-C, Nowakowski, J, Kassel, D.B, Cronin, C.N, McRee, D.E. | | 登録日 | 2003-06-05 | | 公開日 | 2003-08-12 | | 最終更新日 | 2017-08-09 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Structure of a c-Kit Product Complex Reveals the Basis for Kinase Transactivation.
J.Biol.Chem., 278, 2003
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1QPD
 | | STRUCTURAL ANALYSIS OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH NON-SELECTIVE AND SRC FAMILY SELECTIVE KINASE INHIBITORS | | 分子名称: | LCK KINASE, STAUROSPORINE, SULFATE ION | | 著者 | Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M, Zhao, H, Morgenstern, K.A. | | 登録日 | 1999-05-24 | | 公開日 | 2000-05-24 | | 最終更新日 | 2022-12-21 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors.
Structure Fold.Des., 7, 1999
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1QPE
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1QPJ
 | | CRYSTAL STRUCTURE OF THE LYMPHOCYTE-SPECIFIC KINASE LCK IN COMPLEX WITH STAUROSPORINE. | | 分子名称: | LCK TYROSINE KINASE, STAUROSPORINE, SULFATE ION | | 著者 | Zhu, X, Kim, J.L, Rose, P.E, Stover, D.R, Toledo, L.M. | | 登録日 | 1999-05-25 | | 公開日 | 2000-05-31 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors.
Structure Fold.Des., 7, 1999
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2BDF
 | | Src kinase in complex with inhibitor AP23451 | | 分子名称: | Proto-oncogene tyrosine-protein kinase Src, {[(4-{[2-(4-AMINOCYCLOHEXYL)-9-ETHYL-9H-PURIN-6-YL]AMINO}PHENYL)(HYDROXY)PHOSPHORYL]METHYL}PHOSPHONIC ACID | | 著者 | Dalgarno, D, Stehle, T, Schelling, P, Sawyer, T, Narula, S. | | 登録日 | 2005-10-20 | | 公開日 | 2006-10-24 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | 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
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2DQ7
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2BDJ
 | | Src kinase in complex with inhibitor AP23464 | | 分子名称: | 3-[2-(2-CYCLOPENTYL-6-{[4-(DIMETHYLPHOSPHORYL)PHENYL]AMINO}-9H-PURIN-9-YL)ETHYL]PHENOL, Proto-oncogene tyrosine-protein kinase Src | | 著者 | Dalgarno, D, Stehle, T, Schelling, P, Narula, S, Sawyer, T. | | 登録日 | 2005-10-20 | | 公開日 | 2006-10-24 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | 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
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2E2B
 | | Crystal structure of the c-Abl kinase domain in complex with INNO-406 | | 分子名称: | N-[3-(4,5'-BIPYRIMIDIN-2-YLAMINO)-4-METHYLPHENYL]-4-{[(3S)-3-(DIMETHYLAMINO)PYRROLIDIN-1-YL]METHYL}-3-(TRIFLUOROMETHYL) BENZAMIDE, Proto-oncogene tyrosine-protein kinase ABL1 | | 著者 | Horio, T, Hamasaki, T, Wakayama, T, Takagaki, K, Ohgi, T. | | 登録日 | 2006-11-10 | | 公開日 | 2007-05-22 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives
Bioorg.Med.Chem.Lett., 17, 2007
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2B7A
 | | The structural basis of Janus Kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor | | 分子名称: | 2-TERT-BUTYL-9-FLUORO-3,6-DIHYDRO-7H-BENZ[H]-IMIDAZ[4,5-F]ISOQUINOLINE-7-ONE, Tyrosine-protein kinase JAK2 | | 著者 | 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. | | 登録日 | 2005-10-04 | | 公開日 | 2006-01-10 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor.
Blood, 107, 2006
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2EB2
 | | Crystal structure of mutated EGFR kinase domain (G719S) | | 分子名称: | Epidermal growth factor receptor | | 著者 | Yoshikawa, S, Kukimoto-Niino, M, Chen, L, Liu, Z.J, Wang, B.C, Shirouzu, M, Senba, K, Yamamoto, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI) | | 登録日 | 2007-02-06 | | 公開日 | 2008-02-12 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor
Oncogene, 2012
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2EB3
 | | Crystal structure of mutated EGFR kinase domain (L858R) in complex with AMPPNP | | 分子名称: | Epidermal growth factor receptor, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER | | 著者 | Yoshikawa, S, Kukimoto-Niino, M, Shirouzu, M, Senba, K, Yamamoto, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI) | | 登録日 | 2007-02-06 | | 公開日 | 2008-02-12 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.84 Å) | | 主引用文献 | Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor
Oncogene, 2012
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2ETM
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2FGI
 | | CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF FGF RECEPTOR 1 IN COMPLEX WITH INHIBITOR PD173074 | | 分子名称: | 1-TERT-BUTYL-3-[6-(3,5-DIMETHOXY-PHENYL)-2-(4-DIETHYLAMINO-BUTYLAMINO)-PYRIDO[2,3-D]PYRIMIDIN-7-YL]-UREA, PROTEIN (FIBROBLAST GROWTH FACTOR (FGF) RECEPTOR 1) | | 著者 | Mohammadi, M, Froum, S, Hamby, J.M, Schroeder, M, Panek, R.L, Lu, G.H, Eliseenkova, A.V, Green, D, Schlessinger, J, Hubbard, S.R. | | 登録日 | 1998-09-15 | | 公開日 | 1999-09-13 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain.
EMBO J., 17, 1998
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2EVA
 | | Structural Basis for the Interaction of TAK1 Kinase with its Activating Protein TAB1 | | 分子名称: | ADENOSINE, TAK1 kinase - TAB1 chimera fusion protein | | 著者 | Brown, K, Vial, S.C, Dedi, N, Long, J.M, Dunster, N.J, Cheetham, G.M. | | 登録日 | 2005-10-31 | | 公開日 | 2006-05-02 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structural basis for the interaction of TAK1 kinase with its activating protein TAB1
J.Mol.Biol., 354, 2005
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1R0P
 | | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met in complex with the microbial alkaloid K-252a | | 分子名称: | Hepatocyte growth factor receptor, K-252A | | 著者 | Schiering, N, Knapp, S, Marconi, M, Flocco, M.M, Cui, J, Perego, R, Rusconi, L, Cristiani, C. | | 登録日 | 2003-09-22 | | 公開日 | 2003-10-07 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a
Proc.Natl.Acad.Sci.USA, 100, 2003
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8BA4
 | | Crystal structure of JAK2 JH2-V617F in complex with Bemcentinib | | 分子名称: | 1-(3,4-diazatricyclo[9.4.0.0^{2,7}]pentadeca-1(11),2(7),3,5,12,14-hexaen-5-yl)-~{N}3-[(7~{S})-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5~{H}-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine, Tyrosine-protein kinase JAK2 | | 著者 | Haikarainen, T, Silvennoinen, O. | | 登録日 | 2022-10-11 | | 公開日 | 2023-02-01 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Identification of Novel Small Molecule Ligands for JAK2 Pseudokinase Domain.
Pharmaceuticals, 16, 2023
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8BA3
 | | Crystal structure of JAK2 JH2 in complex with Bemcentinib | | 分子名称: | 1-(3,4-diazatricyclo[9.4.0.0^{2,7}]pentadeca-1(11),2(7),3,5,12,14-hexaen-5-yl)-~{N}3-[(7~{S})-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5~{H}-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine, GLYCEROL, Tyrosine-protein kinase JAK2 | | 著者 | Haikarainen, T, Silvennoinen, O. | | 登録日 | 2022-10-11 | | 公開日 | 2023-02-01 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (1.4 Å) | | 主引用文献 | Identification of Novel Small Molecule Ligands for JAK2 Pseudokinase Domain.
Pharmaceuticals, 16, 2023
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8B99
 | | Crystal structure of JAK2 JH2-V617F in complex with JNJ-7706621 | | 分子名称: | 4-({5-amino-1-[(2,6-difluorophenyl)carbonyl]-1H-1,2,4-triazol-3-yl}amino)benzenesulfonamide, GLYCEROL, Tyrosine-protein kinase JAK2 | | 著者 | Haikarainen, T, Silvennoinen, O. | | 登録日 | 2022-10-05 | | 公開日 | 2023-02-01 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Identification of Novel Small Molecule Ligands for JAK2 Pseudokinase Domain.
Pharmaceuticals, 16, 2023
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