From angiotensin ii to cyclic peptides and angiotensin receptor blockers (Arbs): Perspectives of arbs in covid-19 therapy

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Abstract

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.

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Matsoukas, J., Apostolopoulos, V., Zulli, A., Moore, G., Kelaidonis, K., Moschovou, K., & Mavromoustakos, T. (2021, February 1). From angiotensin ii to cyclic peptides and angiotensin receptor blockers (Arbs): Perspectives of arbs in covid-19 therapy. Molecules. MDPI AG. https://doi.org/10.3390/molecules26030618

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