ROCK抑制剂Y-27632对TGF-β1/CTGF通路的影响  

Effects of ROCK inhibitor Y-27632 on TGF-β1/CTGF pathway

作　　者：任杰[1] 安海燕[1] 

机构地区：[1]南方医科大学中医药学院中基文史教研室,广东省广州市510515

出　　处：《世界华人消化杂志》2014年第26期3932-3936,共5页World Chinese Journal of Digestology

基　　金：2013年高等学校博士学科点专项科研基金资助项目;No.20134433120009;省级大学生创新创业训练计划基金资助项目;No.1212113079~~

摘　　要：Y-27632为嘧啶衍生物,是一种近年来合成的特异性Rho相关螺旋卷曲蛋白激酶(Rho associated coiled-coil forming protein kinase,R O C K)抑制剂,能通过调控R O C K介导的多种生物效应从而抑制肝纤维化的形成.研究发现,转化生长因子β1(transforming growth factorβ1,TGF-β1)/结缔组织生长因子(connective tissue growth factor,CTGF)通路参与肝纤维化的形成,TGF-β1诱导其下游效应分子CTGF表达,促使细胞外基质生成增多,导致肝纤维化.Y-27632具有抑制TGF-β1和CTGF表达的作用,本文从ROCK抑制剂Y-27632对TGF-β1/CTGF通路的影响来阐述Y-27632的抗纤维化作用,借此更深入的了解Y-27632的作用靶点,为肝纤维化的靶向治疗提供理论依据.Y-27632, a pyrimidine derivative, is a recently developed synthetic specific inhibitor of Rho associated coiled-coil forming protein kinase （ROCK）, and it inhibits the process of hepatic fi- brosis by regulating a variety of biological effects mediated by ROCK. Recent studies have found that the transforming growth factor β1 （TGF-β1）/ connective tissue growth factor （CTGF） signal- ing pathway is involved in liver fibrosis. TGF-β1 induces the expression of its downstream mol- ecule CTGF, resulting in the increase of extra- cellular matrix and liver fibrosis. Y-27632 can inhibit the expression of TGF-β1 and CTGF. This paper attempts to explain the anti-fibrosis effectof Y-27632 in terms of the impact of Y-27632 on the TGF-β1/CTGF pathway, with an aim to bet- ter understand the functional target of Y-27632 and provide a theoretical basis for the targeted therapy of liver fibrosis.

关 键 词：ROCK抑制剂 Y-27632 肝纤维化 转化生长因子Β1 结缔组织生长因子 

分 类 号：R575.2[医药卫生—消化系统]