以蛋白酶活化受体2为靶点的药物研究进展

Research progress in medicines on protease-activated receptor 2

蛋白酶活化受体2(protease-activated receptor 2,PAR2)是蛋白酶活化受体的成员之一,分布在许多组织和细胞中(如皮肤、呼吸道上皮细胞和胰腺等),具有广泛的生物学效应,参与多种疾病的发生和形成(如机械性疼痛、哮喘、胰腺癌疼痛、炎症和瘙痒等)。调节PAR2活性的相关药物研究有助于发现PAR2在疾病机制中的作用,研发出新的治疗药物。本文主要介绍了PAR2激动剂、拮抗剂及pepducin的研究进展。

Protease-activated receptor 2（PAR2） is a member of protease-activated receptors（PARs）. PAR2 distributed in tissues and cells（such as skin, airway epithelial cell, pancreas, etc.） has a broad biological effects, and is involved in pathogenesis of many diseases, such as mechanical pain, asthma, pain of pancreatic cancer, inflammation, pruritus, etc. Intervention of PAR2 will help us to identify the role of PAR2 in the mechanisms of diseases and in the development of new drugs. This article concentrates on the research progress of agonist, antagonist, and pepducin on PAR2.