《生命科学》 2021, 33(8): 997-1001

PARs在IPF中的作用及其靶向药物研究进展

崔梦奇^1,2 , 任善发^1,2 , 王　明¹ , 高丹迪^1,2 , 肖　婷^1,* , 周红刚^1,2,* , 杨　诚^1,2,*

¹南开大学药物化学生物学国家重点实验室，南开大学药学院和天津市分子药物研究重点实验室， 天津 300457 ²天津市国际生物医药联合研究院高通量分子筛选中心，天津 300350

摘　要：

特发性肺纤维化(idiopathic pulmonary fibrosis, IPF) 是一种病因不明的慢性、进行性、纤维化性间质性肺炎，治愈率低而死亡率很高，目前有效的治疗药物较为匮乏。蛋白酶激活受体(protease activated receptors, PARs) 的不可逆地激活对维持肺功能具有重要作用，PARs 的异常表达与活化可促进炎症和纤维化过程。因此，在特发性肺纤维化的治疗中，靶向PARs 可能成为一种新的治疗手段。该文介绍了PARs 在促进特发性肺纤维化进程中的功能及作用机制，并且总结了靶向PARs 的抗肺纤维化药物的研究进展。

通讯作者：肖　婷 , Email:xting2011@163.com 周红刚 , Email:honggang.zhou@nankai.edu.cn 杨　诚 , Email:cheng.yang@ nankai.edu.cn

The role of protease activated receptors in idiopathic pulmonary fibrosis and the advance in its targeted drugs

CUI Meng-Qi^1,2 , REN Shan-Fa^1,2 , WANG Ming¹ , GAO Dan-Di^1,2 , XIAO Ting^1,* , ZHOU Hong-Gang^1,2,* , YANG Cheng^1,2,*

¹State Key Laboratory of Medicinal Chemical Biology, Nankai University School of Pharmacy, Nankai University and Tianjin Key Laboratory of Molecular Drug Research, Tianjin 300457, China ²High-throughput Molecular Screening Center of Tianjin International Joint Research Institute of Biomedicine, Tianjin 300350, China

Abstract:

Idiopathic pulmonary fibrosis is a chronic, progressive, fibrotic interstitial pneumonia of unknown etiology. The cure rate is low and the mortality rate is high. At present, effective treatment drugs are scarce. Irreversible activation of PARs plays an important role in maintaining pulmonary function, and abnormal expression and activation of PARs can promote the process of inflammation and idiopathic pulmonary fibrosis. Therefore, targeted PARs may be a new therapeutic method in the treatment of idiopathic pulmonary fibrosis. This paper introduces the function and mechanism of PARs in promoting idiopathic pulmonary fibrosis, and summarizes the advance in anti-fibrosis drugs targeting PARs.

Communication Author：XIAO Ting , Email:xting2011@163.com ZHOU Hong-Gang , Email:honggang.zhou@nankai.edu.cn YANG Cheng , Email:cheng.yang@ nankai.edu.cn