Progress in researches about focal adhesion kinase in gastrointestinal tract.
Focal adhesion kinase (FAK) is a 125-kDa non-receptor protein tyrosine. Growth factors or the clustering of integrins facilitate the rapid phosphorylation of FAK at Tyr-397 and this in turn recruits Src-family protein tyrosine kinases, resulting in the phosphorylation of Tyr-576 and Tyr-577 in the FAK activation loop and full catalytic FAK activation. FAK plays a critical role in the biological processes of normal and cancer cells including the gastrointestinal tract. FAK also plays an important role in the restitution, cell survival and apoptosis and carcinogenesis of the gastrointestinal tract. FAK is over-expressed in cancer cells and its over-expression and elevated activities are associated with motility and invasion of cancer cells. FAK has been proposed as a potential target in cancer therapy. Small molecule inhibitors effectively inhibit the kinase activity of FAK and show a potent inhibitory effect for the proliferation and migration of tumor cells, indicating a high potential for application in cancer therapy.
Hao
Hui-Fang
HF
Department of Gastroenterological Surgery, Transplantation and Surgical Oncology, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, Okayama 700-8558, Japan.
Naomoto
Yoshio
Y
Bao
Xiao-Hong
XH
Watanabe
Nobuyuki
N
Sakurama
Kazufumi
K
Noma
Kazuhiro
K
Tomono
Yasuko
Y
Fukazawa
Takuya
T
Shirakawa
Yasuhiro
Y
Yamatsuji
Tomoki
T
Matsuoka
Junji
J
Takaoka
Munenori
M
D000818:Animals; D017209:Apoptosis / Q000502:physiology; D002470:Cell Survival; D004791:Enzyme Inhibitors / Q000627:therapeutic use; D051416:Focal Adhesion Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D005770:Gastrointestinal Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D041981:Gastrointestinal Tract / Q000201:enzymology* / Q000473:pathology; D006801:Humans; D015398:Signal Transduction / Q000502:physiology
D004791:Enzyme Inhibitors; D051416:Focal Adhesion Protein-Tyrosine Kinases