以αv为靶向的整合素作为肺纤维化的药物靶点  

Integrins targetingαv are used as drug targets for pulmonary fibrosis

作　　者：刘南玉 岳红梅[1,2] 宋佩佩[1] 魏继芳 魏雅倩 谢莹莹 王嘉琪 LIU Nanyu;YUE Hongmei;SONG Peipei;WEI Jifang;WEI Yaqian;XIE Yingying;WANG Jiaqi(The First Clinical Medical College of Lanzhou University,Lanzhou 730000,Gansu,China;Department of Respiratory Medicine,the First Hospital of Lanzhou University,Lanzhou 730000,Gansu,China)

机构地区：[1]兰州大学第一临床医学院,甘肃兰州730000 [2]兰州大学第一医院呼吸内科,甘肃兰州730000

出　　处：《中国临床药理学与治疗学》2022年第6期709-714,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：甘肃省科技计划项目(18YF1FA106)。

摘　　要：特发性肺纤维化是一种病因不明、预后不良的慢性进行性间质性肺疾病,尽管接受了治疗,大多数患者病情仍有可能进展或恶化。整合素是异二聚体细胞表面蛋白,是干预肺纤维化有希望的治疗靶点。αv整合素是纤维化发展的核心,因为它们激活潜伏的TGF-β,一种已知的促纤维化细胞因子。αv亚基可以与β1、β3、β5、β6或β8亚基形成异二聚体,这些整合素中的一种或多种对于肺纤维化的发展至关重要,但尚不清楚它们的相对重要性。本综述总结了肺纤维化与αv整合素相关联的知识,以及有关αv整合素抑制剂的新出现的临床前研究和临床试验。IPF is a chronic progressive interstitial lung disease of unknown etiology and poor prognosis,and despite receive treatment,most patients consideration are likely to progress or worsen.Integrins are heterodimer cell surface proteins that are promising therapeutic targets for intervention in pulmonary fibrosis.Alphav integrins are central to the development of fibrosis because they activate latent TGF-β,a known pro-fibrosis cytokine.The alphav subunit may form heterodimers with theβ1,β3,β5,β6,orβ8 subunits,one or more of which are essential for the development of pulmonary fibrosis,but their relative importance is unclear.This review summarizes the knowledge of the association of pulmonary fibrosis with alpha-val-integrins,as well as emerging preclinical studies and clinical trials of alpha-fibrosis inhibitors.

关 键 词：肺纤维化 αv整合素 TGF-Β αv整合素抑制剂 

分 类 号：R563[医药卫生—呼吸系统]