成纤维细胞生长因子受体及相关抗肿瘤靶向药物的研究进展

Research Progress on Fibroblast Growth Factor Receptors in Cancer and Antitumor Targeting Drugs

成纤维细胞生长因子受体(FGFR)作为受体酪氨酸激酶超家族的成员,通过调控细胞的增殖、分化和存活,对胚胎发育、组织修复及代谢调控等生理功能发挥重要作用。FGFR基因扩增、基因突变、基因融合引起的表达及调控异常与多种癌症发生发展有关,因而,FGFR成为癌症治疗中一个重要的潜在靶点。目前针对FGFR的靶向药物研究及应用取得实质性进展,其中一些药物已被批准用于临床治疗或处于临床试验阶段。概述FGFR家族,总结FGFR在肿瘤中的异常表达以及FGFR靶向药物的发展。

Fibroblast growth factor receptors(FGFRs)belong to a large superfamily of receptor tyrosine kinases.FGFR signaling participates in key cellular activities such as cell proliferation,differentiation and survival,and plays crucial roles in multiple physiological processes during embryonic development,adult tissue repair and metabolic regulation.Dysregulation of FGFR caused by gene amplification,gene mutation and gene fusion has also been implicated in many types of human cancers.Therefore,FGFR has become a promising potential target in cancer treatment.Currently,substantial progress has been made in the research and application of targeting drugs for FGFR,some of which have been approved for clinical treatment or are under clinical trials.Collectively,the FGFR family members,its abnormal expression in tumors,and the development of drugs targeting FGFR are summarized in the present article.