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焦点黏附激酶作为癌症治疗靶点。

Focal adhesion kinase as a cancer therapy target.

机构信息

Department of Surgical Oncology, Roswell Park Cancer Institute, Buffalo, NY 14263, USA.

出版信息

Anticancer Agents Med Chem. 2010 Dec;10(10):735-41. doi: 10.2174/187152010794728648.

Abstract

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that resides at the sites of focal adhesions. The 125 kDa FAK protein is encoded by the FAK gene located on human chromosome 8q24. Structurally, FAK consists of an amino-terminal regulatory FERM domain, a central catalytic kinase domain, and a carboxy-terminal focal adhesion targeting domain. FAK has been shown to be an important mediator of cell adhesion, growth, proliferation, survival, angiogenesis and migration, all of which are often disrupted in cancer cells. Normal tissues have low expression of FAK, while primary and metastatic tumors significantly overexpress this protein. This review summarizes expression of FAK by immunohistochemical staining in different tumor types and presents several FAK inhibition therapy approaches.

摘要

黏着斑激酶(FAK)是一种非受体酪氨酸激酶,位于黏着斑部位。125 kDa 的 FAK 蛋白由位于人类染色体 8q24 上的 FAK 基因编码。结构上,FAK 由氨基端调节 FERM 结构域、中央催化激酶结构域和羧基端黏着斑靶向结构域组成。FAK 已被证明是细胞黏附、生长、增殖、存活、血管生成和迁移的重要介质,所有这些在癌细胞中经常受到干扰。正常组织中 FAK 的表达水平较低,而原发性和转移性肿瘤显著过表达这种蛋白。本文通过免疫组织化学染色综述了 FAK 在不同肿瘤类型中的表达,并介绍了几种 FAK 抑制治疗方法。

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