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Kinins and peptide receptors

  • Domenico Regoli EMAIL logo and Fernand Gobeil
Published/Copyright: September 25, 2015

Abstract

This paper is divided into two sections: the first contains the essential elements of the opening lecture presented by Pr. Regoli to the 2015 International Kinin Symposium in S. Paulo, Brazil on June 28th and the second is the celebration of Dr. Regoli’s 60 years of research on vasoactive peptides. The cardiovascular homeostasis derives from a balance of two systems, the renin-angiotensin system (RAS) and the kallikrein-kinin system (KKS). The biologically active effector entity of RAS is angiotensin receptor-1 (AT-1R), and that of KKS is bradykinin B2 receptor (B2R). The first mediates vasoconstriction, the second is the most potent and efficient vasodilator. Thanks to its complex and multi-functional mechanism of action, involving nitric oxide (NO), prostacyclin and endothelial hyperpolarizing factor (EDHF). B2R is instrumental for the supply of blood, oxygen and nutrition to tissues. KKS is present on the vascular endothelium and functions as an autacoid playing major roles in cardiovascular diseases (CVDs) and diabetes. KKS exerts a paramount role in the prevention of thrombosis and atherosclerosis. Such knowledge emphasizes the already prominent value of the ACE-inhibitors (ACEIs) for the treatment of CVDs and diabetes. Indeed, the ACEIs, thanks to their double action (block of the RAS and potentiation of the KKS) are the ideal agents for a rational treatment of these diseases.


Corresponding author: Domenico Regoli, Department of Medical Sciences, University of Ferrara, Ferrara, Italy; and Faculty of Medicine and Health Sciences, Department of Pharmacology and Physiology, Université de Sherbrooke, Québec, J1H 5N4 Canada, e-mail:

Acknowledgments

I wish to thank the students who have contributed to the work on KKS in my lab. This list mentions only the students who got their PhD and the chemists: Jean Barabé, Francis Rioux, François Marceau, Réjean Couture, Pierrette Gaudreault, Pedro D’Orléans-Juste, Guy Drapeau, Nour-Eddine Rhaleb, Daniella Jukic, and the co-author of this paper Fernand Gobeil; chemists: Van Kil Park, Serge Saint-Pierre, and Witold Neugebauer.

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Received: 2015-9-3
Accepted: 2015-9-23
Published Online: 2015-9-25
Published in Print: 2016-4-1

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