From Angiotensin II to Cyclic Peptides and Angiotensin Receptor Blockers (ARBs): Perspectives of ARBs in COVID-19 Therapy

Molecules

Kalliopi Moschovou¹  Thomas Mavromoustakos¹  Anthony Zulli²  Vasso Apostolopoulos²  John Matsoukas²  Konstantinos Kelaidonis³  Graham Moore⁴ 

[1] Department of Chemistry, National and Kapodistrian University of Athens, Zographou, 15784 Athens, Greece;Institute for Health and Sport, Victoria University, Melbourne, VIC 3030, Australia;NewDrug, P.C., Patras Science Park, 26504 Patras, Greece;Pepmetics Inc., 772 Murphy Place, Victoria, BC V8Y 3H4, Canada;

关键词: angiotensin II;    RAS;    cyclic peptides;    Sarmesin;    Sartans;    mimetics;   

DOI  :  10.3390/molecules26030618

来源: DOAJ

【 摘 要 】

The octapeptide hormone angiotensin II is one of the most studied peptides with the aim of designing and synthesizing non-peptide mimetics for oral administration. To achieve this, cyclizations at different positions within the peptide molecule has been a useful strategy to define the active conformation. These studies on angiotensin II led to the discovery of Sarmesin, a type II angiotensin II antagonist, and the breakthrough non-peptide mimetic Losartan, the first in a series of sartans marketed as a new generation of anti-hypertensive drugs in the 1990s. Angiotensin II receptor blockers (ARBS) and angiotensin I converting enzyme inhibitors (ACEI) were recently reported to protect hypertensive patients infected with SARS-CoV-2. The renin–angiotensin system (RAS) inhibitors reduce excess angiotensin II and increase antagonist heptapeptides alamandine and aspamandine which counterbalance angiotensin II and maintain homeostasis and vasodilation.

【 授权许可】

Unknown