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Therapeutic targeting of the angiotensin-converting enzyme 2/Angiotensin-(1-7)/Mas cascade in the renin-angiotensin system: a patent review

Item Type:Review
Title:Therapeutic targeting of the angiotensin-converting enzyme 2/Angiotensin-(1-7)/Mas cascade in the renin-angiotensin system: a patent review
Creators Name:Ferreira, A.J. and Bader, M. and Santos, R.A.S.
Abstract:Introduction: The renin-angiotensin system (RAS) is a main therapeutic target for cardiovascular diseases. Within the last two decades, novel components of the RAS have been discovered, opening new opportunities to interfere with its activity. Angiotensin(Ang)-(1-7) is synthesized by angiotensin-converting enzyme 2 (ACE2), and interacts with the G-protein-coupled receptor Mas. The axis formed by ACE2/Ang-(1-7)/Mas represents an endogenous counter regulatory pathway within the RAS. Areas covered: In this review, the authors discuss patents and recent initiatives to develop therapeutic strategies based on the ACE2/Ang-(1-7)/Mas axis. Expert opinion: Many publications and patents support a strategy to interfere with the activity of the RAS by stimulating its counter-regulatory axis mainly in two different ways: i) To increase the activity of ACE2, which will impact the system by increasing the inactivation of Ang II and the production of Ang-(1-7); ii) To stimulate Mas, taking advantage of nanostructured formulations of the natural peptide or analogues of Ang-(1-7). Although the preclinical studies are compelling, the possible impact of these novel therapeutic tools for the treatment of cardiometabolic diseases will only be known after completion of the ongoing clinical studies.
Keywords:ACE2 Activators, Angiotensin II, Angiotensin-(1-7) Formulations, Cardiovascular Diseases, Mas Agonists, Animals
Source:Expert Opinion on Therapeutic Patents
ISSN:1354-3776
Publisher:Informa Healthcare (U.K.)
Volume:22
Number:5
Page Range:567-574
Date:May 2012
Official Publication:https://doi.org/10.1517/13543776.2012.682572
PubMed:View item in PubMed

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