拮抗结缔组织生长因子小分子化合物的研究进展  

Research Progress on Small-molecule Compounds against Connective Tissue Growth Factor

作　　者：刘俊丽 张沐新[1] 梁迪[1] 郑明昕 周小平[1] LIU Jun-li;ZHANG Mu-xin;LIANG Di;ZHENG Ming-xin;ZHOU Xiao-ping(Department of Medicinal Chemistry, School of Pharmacy, Jilin University, Jilin Changchun 130021, China)

机构地区：[1]吉林大学药学院药物化学教研室,吉林长春130021

出　　处：《中国药物警戒》2018年第2期98-102,共5页Chinese Journal of Pharmacovigilance

基　　金：国家自然科学基金项目(31270851):重组谷胱甘肽过氧化物酶及其双功能抗氧化酶的筛选与表达;吉林省卫生计生委项目(2016J063):具有抗癌作用的分蘖葱头多糖的研究;吉林省科技发展计划项目(20180414075GH):COX/5-LOX多靶点抑制剂的合成及其抗肝纤维化作用研究

摘　　要：目的对拮抗结缔组织生长因子(CTGF)小分子化合物进行综述和分析。方法对近年来国内外发表的针对现有的药物和新型结构类型化合物研究能够拮抗CTGF的小分子化合物的文献进行总结与分析。结果拮抗CTGF的小分子化合物的研究可以分为两个部分:一部分是针对现有的药物或天然产物展开的;另一部分是一系列不同结构类型的小分子化合物。结论 CTGF作为生物体内重要的细胞因子,只在间质细胞中表达,主要介导TGF-β的促纤维化作用,是一个更有效和特异的抗纤维化作用的靶点,虽然仅有几种结构类型,但是也开启了能够拮抗CTGF小分子化合物研究的序幕。Objective To provide a concise overview of small molecule connective tissue growth factor(CTGF)inhibitors.Methods A summarization of the small molecules was provided,both the approved drugs and the agents under developing with new structures,that can inhibit CTGF.Results The research on small molecule CTGF inhibitors could be mainly classified into two categories:one is based on the approved drugs or natural products,the other is the small molecule compounds with new structures.Conclusion As a very important cytokine which is only expressed in interstitial cells,CTGF,inducing the fibrosis of TGF-β,is an effective and specific target for anti-fibrosis cytokine in organism.There are only a few structural types of compounds reported,but they will also be the prelude to provide useful references for developing more potential small molecule CTGF inhibitors in the future.

关 键 词：结缔组织生长因子 组织纤维化 小分子化合物 

分 类 号：R965[医药卫生—药理学]