抗肿瘤药物Raf激酶抑制剂的研究进展

Advances in the research of the anti-cancer agent-Raf kinase inhibitor

随着分子生物学的发展,对基于肿瘤分子机制研究的肿瘤分子靶向治疗的研究已获重大进展。蛋白激酶抑制剂是目前肿瘤靶向治疗药物研究的重点之一,通过阻碍细胞内分子传导通路,影响肿瘤细胞的存活、增殖以及疾病进展。在Raf/MEK/ERK信号传导通路中,Raf激酶发挥着至关重要的作用,Raf激酶的突变能使ERK通路保持激活状态,这最终导致细胞的增殖和分化。本综述将阐述Raf激酶在正常与肿瘤细胞中的功能并重点关注于近期发表的各种类型Raf激酶抑制剂。

Advances in the understanding of cancer at the molecular level have led to much progresses in the development of anti-cancer agents. Among the newly inhibitors target intracellular molecules crucial in si invented medications for gnaling targeted cancer therapy, protein kinase pathways for cancer cell survival, proliferation, and dis- ease progression. The Raf kinases are pivotal molecules within the Raf/mitogen extracellular kinase（MEK）/extracel- lular signal-related kinase（ERK） signaling pathway. Mutations of Raf kinase lead to a constitutive activation of the ERK pathway, which ultimately results in increased cell division, and cell survival. This review article focused on the function of Raf kinase in normal and tumor cells related to ERK pathway inhibitors ,with a particular emphasis on Raf kinase inhibitors which was recently approved in recent literatures.