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粘着斑激酶抑制剂,对癌症的有力一击。

Focal adhesion kinase inhibitors, a heavy punch to cancer.

作者信息

Wu Yueling, Li Ning, Ye Chengfeng, Jiang Xingmei, Luo Hui, Zhang Baoyuan, Zhang Ying, Zhang Qingyu

机构信息

Department of Obstetrics and Gynecology, Affiliated Hospital of Guangdong Medical University, Zhanjiang, 524001, China.

Graduate School of Guangdong Medical University, Zhanjiang, 524023, China.

出版信息

Discov Oncol. 2021 Nov 22;12(1):52. doi: 10.1007/s12672-021-00449-y.

Abstract

Kinases are the ideal druggable targets for diseases and especially were highlighted on cancer therapy. Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase and its aberrant signaling extensively implicates in the progression of most cancer types, involving in cancer cell growth, adhesion, migration, and tumor microenvironment (TME) remodeling. FAK is commonly overexpressed and activated in a variety of cancers and plays as a targetable kinase in cancer therapy. FAK inhibitors already exhibited promising performance in preclinical and early-stage clinical trials. Moreover, substantial evidence has implied that targeting FAK is more effective in combination strategy, thereby reversing the failure of chemotherapies or targeted therapies in solid tumors. In the current review, we summarized the drug development progress, chemotherapy strategy, and perspective view for FAK inhibitors.

摘要

激酶是治疗疾病的理想可成药靶点,在癌症治疗中尤为突出。粘着斑激酶(FAK)是一种非受体酪氨酸激酶,其异常信号传导广泛涉及大多数癌症类型的进展,包括癌细胞的生长、粘附、迁移以及肿瘤微环境(TME)重塑。FAK在多种癌症中通常过度表达并被激活,在癌症治疗中作为一个可靶向的激酶发挥作用。FAK抑制剂在临床前和早期临床试验中已显示出有前景的效果。此外,大量证据表明,在联合治疗策略中靶向FAK更有效,从而扭转实体瘤化疗或靶向治疗的失败局面。在本综述中,我们总结了FAK抑制剂的药物研发进展、化疗策略以及前景展望。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e2af/8777493/fa4020cd6764/12672_2021_449_Fig1_HTML.jpg

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