Co-crystal structures of PTK6: With Dasatinib at 2.24 Å, with novel imidazo[1,2-a]pyrazin-8-amine derivative inhibitor at 1.70 Å resolution

Human Protein tyrosine kinase 6 (PTK6)(EC:2.7.10.2), also known as the breast tumor kinase (BRK), is an intracellular non-receptor Src-related tyrosine kinase expressed five-fold or more in human breast tumors and breast cancer cell lines but its expression being low or completely absent from normal...

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Veröffentlicht in:	Biochemical and biophysical research communications 2017-01, Vol.482 (4), p.1289-1295
Hauptverfasser:	Thakur, Manish Kumar, Birudukota, Swarnakumari, Swaminathan, Srinivasan, Battula, Sivarama Krishna, Vadivelu, Sarvanan, Tyagi, Rajiv, Gosu, Ramachandraiah
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES Adenosine Triphosphate - chemistry AMINES Amines - chemistry Breast Neoplasms - drug therapy Breast Neoplasms - metabolism BRK Catalytic Domain Cloning, Molecular Co-crystal structure Crystallography, X-Ray Dasatinib Dasatinib - chemistry Diffusion Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Female Humans Imidazoles - chemistry INHIBITION Inhibitor Inhibitory Concentration 50 MAMMARY GLANDS Neoplasm Proteins - chemistry NEOPLASMS PHOSPHOTRANSFERASES Protein Binding Protein Domains Protein Interaction Mapping Protein-Tyrosine Kinases - chemistry PTK6 RESOLUTION TEMPERATURE RANGE 0273-0400 K Tyrosine kinase X RADIATION X-RAY DIFFRACTION
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