Department of Pharmacy, Royal Prince Alfred Hospital, Sydney, Australia.
School of Molecular Science, College of Science, La Trobe University, Melbourne, Australia.
Clin Sci (Lond). 2020 Dec 11;134(23):3137-3158. doi: 10.1042/CS20201268.
Twenty years ago, the discovery of angiotensin-converting enzyme 2 (ACE2) was an important breakthrough dramatically enhancing our understanding of the renin-angiotensin system (RAS). The classical RAS is driven by its key enzyme ACE and is pivotal in the regulation of blood pressure and fluid homeostasis. More recently, it has been recognised that the protective RAS regulated by ACE2 counterbalances many of the deleterious effects of the classical RAS. Studies in murine models demonstrated that manipulating the protective RAS can dramatically alter many diseases including liver disease. Liver-specific overexpression of ACE2 in mice with liver fibrosis has proved to be highly effective in antagonising liver injury and fibrosis progression. Importantly, despite its highly protective role in disease pathogenesis, ACE2 is hijacked by SARS-CoV-2 as a cellular receptor to gain entry to alveolar epithelial cells, causing COVID-19, a severe respiratory disease in humans. COVID-19 is frequently life-threatening especially in elderly or people with other medical conditions. As an unprecedented number of COVID-19 patients have been affected globally, there is an urgent need to discover novel therapeutics targeting the interaction between the SARS-CoV-2 spike protein and ACE2. Understanding the role of ACE2 in physiology, pathobiology and as a cellular receptor for SARS-CoV-2 infection provides insight into potential new therapeutic strategies aiming to prevent SARS-CoV-2 infection related tissue injury. This review outlines the role of the RAS with a strong focus on ACE2-driven protective RAS in liver disease and provides therapeutic approaches to develop strategies to prevent SARS-CoV-2 infection in humans.
二十年前,血管紧张素转换酶 2(ACE2)的发现是一个重要的突破,极大地提高了我们对肾素-血管紧张素系统(RAS)的理解。经典的 RAS 由其关键酶 ACE 驱动,在调节血压和液体平衡中起着至关重要的作用。最近,人们认识到,ACE2 调节的保护性 RAS 抵消了经典 RAS 的许多有害影响。在鼠模型中的研究表明,操纵保护性 RAS 可以显著改变许多疾病,包括肝病。在纤维化的小鼠中,肝脏特异性过表达 ACE2 已被证明在拮抗肝损伤和纤维化进展方面非常有效。重要的是,尽管 ACE2 在疾病发病机制中具有高度保护作用,但它被 SARS-CoV-2 劫持为细胞受体,进入肺泡上皮细胞,导致 COVID-19,这是一种严重的人类呼吸道疾病。COVID-19 经常危及生命,尤其是在老年人或有其他医疗条件的人身上。由于全球受 COVID-19 影响的人数空前,因此迫切需要发现针对 SARS-CoV-2 刺突蛋白和 ACE2 相互作用的新型治疗方法。了解 ACE2 在生理学、病理生理学以及作为 SARS-CoV-2 感染的细胞受体中的作用,为潜在的新治疗策略提供了深入的了解,这些策略旨在预防 SARS-CoV-2 感染相关的组织损伤。本综述概述了 RAS 的作用,重点介绍了 ACE2 驱动的保护性 RAS 在肝病中的作用,并提供了治疗方法来开发预防人类 SARS-CoV-2 感染的策略。