髓过氧化物酶抑制剂的研究进展  

Research progress on the development of myeloperoxidase inhibitors

作　　者：王玉婷 秦亚娟[1] 厉廷有[1] WANG Yuting;QIN Yajuan;LI Tingyou(School of Pharmacy,Nanjing Medical University,Nanjing 211166,China)

机构地区：[1]南京医科大学药学院,江苏南京211166

出　　处：《南京医科大学学报（自然科学版）》2023年第12期1756-1763,共8页Journal of Nanjing Medical University(Natural Sciences)

基　　金：国家自然科学基金(81573280,81803349)。

摘　　要：髓过氧化物酶(myeloperoxidase,MPO)是血红素过氧化物酶⁃环氧化酶超家族的重要成员。MPO在多种炎症细胞,包括中性粒细胞、活化的小胶质细胞和单核/巨噬细胞等,以及星形胶质细胞和神经元中表达,在免疫监视和宿主防御机制中起着重要作用。然而,研究发现MPO的表达和活性的增加与包括帕金森病、阿尔茨海默病、脑卒中、心血管疾病等多种重大疾病的发生和进展相关。多年来,多家医药公司和科研单位在MPO抑制剂的研发中取得大量进展,文章综述了MPO蛋白的结构、催化机制、抑制剂的研发进展等,旨在为MPO抑制剂的研发提供参考。Myeloperoxidase(MPO)is an important member of the haemoglobin peroxidase⁃cyclooxygenase superfamily.It is expressed in a variety of inflammatory cells,including neutrophils,activated microglia,monocytes/macrophages,as well as astrocytes and neurons,and plays an important role in immune surveillance and host defense mechanisms.However,studies have found that the increased expression and activity of MPO is associated with the development and progression of several major diseases,including Parkinson’s disease,Alzheimer’s disease,stroke,and cardiovascular disease.Over the years,several pharmaceutical companies and research institutes have made a lot of progress in the development of MPO inhibitors.This review mainly summrizes the structure of MPO protein,its catalytic mechanism and the progress of inhibitor development,aiming to provide a reference for the development of this enzyme inhibitors.

关 键 词：髓过氧化物酶 蛋白结构 催化机制 可逆抑制剂 不可逆抑制剂 

分 类 号：R914.4[医药卫生—药物化学]