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Progress in researches about focal adhesion kinase in gastrointestinal tract

机译:胃肠道粘着斑激酶的研究进展

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摘要

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.
机译:黏着斑激酶(FAK)是一种125 kDa的非受体蛋白酪氨酸。生长因子或整联蛋白的聚集促进TAK-397处FAK的快速磷酸化,这反过来募集Src家族蛋白酪氨酸激酶,导致FAK激活环中Tyr-576和Tyr-577的磷酸化以及完全催化的FAK激活。 FAK在正常细胞和包括胃肠道在内的癌细胞的生物过程中起着至关重要的作用。 FAK在胃肠道的恢复,细胞​​存活以及凋亡和癌变中也起重要作用。 FAK在癌细胞中过表达,其过表达和活性升高与癌细胞的活力和侵袭有关。 FAK已被提议作为癌症治疗中的潜在靶标。小分子抑制剂有效抑制FAK的激酶活性,并显示出对肿瘤细胞增殖和迁移的有效抑制作用,表明在癌症治疗中具有很高的应用潜力。

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