酪氨酸激酶
蛋白激酶结构域
激酶
原癌基因酪氨酸蛋白激酶Src
受体酪氨酸激酶
化学
生物
分子生物学
细胞生物学
基因
生物化学
信号转导
突变体
作者
Manish K. Thakur,Amit Kumar,Swarnakumari Birudukota,Srinivasan Swaminathan,Rajiv Tyagi,Ramachandraiah Gosu
标识
DOI:10.1016/j.bbrc.2016.07.121
摘要
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 in a majority of human breast tumors and breast cancer cell lines, but its expression is low or completely absent in normal mammary glands. In the recent past, several studies have suggested that PTK6 is a potential therapeutic target in cancer. To understand its structural and functional properties, the PTK6 kinase domain (PTK6-KD) gene was cloned, overexpressed in a baculo-insect cell system, purified and crystallized at room temperature. X-ray diffraction data to 2.33 Å resolution was collected on a single PTK6-KD crystal, which belonged to the triclinic space group P1. The Matthews coefficient calculation suggested the presence of four protein molecules per asymmetric unit, with a solvent content of ∼50%.The structure has been solved by molecular replacement and crystal structure data submitted to the protein data bank under the accession number 5D7V. This is the first report of apo PTK6-KD structure crystallized in DFG-in and αC-helix-out conformation.
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