In addition, the classical RAS driven by ACE has been shown to be associated with a variety of diseases such as chronic heart disease, kidney disease and diabetes ( Warner et al., 2020).Īngiotensin-converting-enzyme inhibitors (ACE inhibitors, ACEIs) are widely used to lower blood pressure and reduce cardiac oxygen consumption ( Herman et al., 2021). The main function of ACE is to convert the hormone angiotensin I into active angiotensin II ( Turner and Hooper, 2002 Fukuda and Sata, 2008) and to degrade bradykinin (a vasodilator), which constricts blood vessels and leads to an increase in blood pressure. In this review, we have summarized the research advances of ACE inhibitors, focusing on the development sources, design strategies and analysis of structure-activity relationships and the biological activities of ACE inhibitors. In recent years, researchers have attempted to reduce the adverse effects of ACEIs by improving the selectivity of ACEIs for structural domains based on conformational relationships, and have developed a series of novel ACEIs. Nevertheless, ACEIs are associated with a range of adverse effects such as renal insufficiency, which limits their use. Angiotensin-converting-enzyme inhibitors (ACE inhibitors, ACEIs) decrease the formation of angiotensin II and increase the level of bradykinin, thus relaxing blood vessels as well as reducing blood volume, lowering blood pressure and reducing oxygen consumption by the heart, which can be used to prevent and treat cardiovascular diseases and kidney diseases. It degrades bradykinin and other vasoactive peptides. 4Department of Pharmacy, Chengdu Fifth People’s Hospital, Chengdu, ChinaĪngiotensin-converting enzyme (ACE), a zinc metalloprotein, is a central component of the renin–angiotensin system (RAS). ![]()
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