摘要
成纤维细胞生长因子21(Fibroblast growth factor 21,FGF21)是由181个氨基酸组成的内分泌因子,能与β-klotho和成纤维细胞生长因子受体(Fibroblast growth factorreceptor,FGFR)形成复合物激活下游信号,参与机体物质代谢、维持脂肪和糖代谢的平衡。FGF21与非酒精性脂肪肝病、肥胖和糖尿病等疾病密切相关,其水平在不同疾病中有不同的变化,外源给予FGF21对不同疾病有一定的治疗作用。FGF21存在半衰期短、稳定性差的问题,影响了其在临床中的运用。目前虽无批准的FGF21药物上市,但已有Efruxifermin、Pegbelfermin、BIO89-100等能延长半衰期的FGF21类药物在临床试验中表现出良好效果。文章总结了FGF21的生物学功能、FGF21水平在相关疾病中的改变和作用、以及FGF21在研药物的新进展,旨在为FGF21及其类似物的开发提供有效信息。
Fibroblast growth factor 21(FGF21)is an endocrine factor,which is composed of 181 amino acids.It can form a complex withβ-klotho and fibroblast growth factor receptor(FGFR).The complex can activate downstream signals,participate in body metabolism,maintain fat and glucose homeostasis.FGF21 is closely related to nonalcoholic fatty liver disease,obesity and diabetes,and its level varies in different diseases.Exogenous administration of FGF21 has a certain therapeutic effect on different diseases.FGF21 has the problems of short half-life and poor stability,which limits its clinical application.Although there are no approved FGF21 drugs on the market,some drugs that can prolong the half-life of FGF21,such as Efruxifermin,Pegbelfermin and BIO89-100,have shown good results in clinical trials.This paper summarizes the biological function of FGF21,the change and role of FGF21 in related diseases,and the new progress of FGF21 in drug research,in order to provide effective information for the development of FGF21 and its analogues.
作者
徐赛
戴佳
童玥
XU Sai;DAI Jia;TONG Yue(Jiangsu Key Laboratory of Druggability of Biopharmaceuticals,China Pharmaceutical University,Nanjing 210009,China;School of Life Science and Technology,China Pharmaceutical University,Nanjing 210009,China)
出处
《药物生物技术》
CAS
2022年第2期209-216,共8页
Pharmaceutical Biotechnology
