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The development of myeloperoxidase inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-11-15 , DOI: 10.1016/j.bmcl.2018.11.031
Semira Galijasevic

Myeloperoxidase (MPO), an abundant hemoprotein present in neutrophils and monocytes, plays a significant role in immune surveillance and host defense mechanisms. However, increased MPO activity has been linked to a number of pathologies with compelling evidence in initiation and progression of inflammatory events. As a result, search for active compounds that can efficiently inhibit MPO activity and subsequently decrease inflammatory events has been focus of the current research.

This perspective provides an overview of the development of MPO inhibitors, their mechanism of action and the review of molecules that were in clinical trials as promising MPO inhibitors.



中文翻译:

髓过氧化物酶抑制剂的开发

髓过氧化物酶(MPO)是一种在中性粒细胞和单核细胞中存在的丰富血红蛋白,在免疫监视和宿主防御机制中起着重要作用。然而,增加的MPO活性与多种病理学有关,在炎症事件的发生和发展中具有令人信服的证据。结果,寻找能够有效抑制MPO活性并随后减少炎症事件的活性化合物一直是当前研究的重点。

该观点概述了MPO抑制剂的开发,它们的作用机理以及在临床试验中作为有前途的MPO抑制剂的分子的综述。

更新日期:2018-11-15
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