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Updated: Apr 3, 2026

A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors
Published on: December 2, 2022
The kallikrein-kinin system (KKS), through bradykinin B2 receptor (B2R), is a potent vasodilator crucial for cardiovascular homeostasis. KKS and ACE inhibitors offer a dual approach to treating cardiovascular diseases and diabetes.
Area of Science:
- Cardiovascular Physiology
- Pharmacology
Background:
- Cardiovascular homeostasis relies on the balance between the renin-angiotensin system (RAS) and the kallikrein-kinin system (KKS).
- The bradykinin B2 receptor (B2R), the effector of KKS, is a potent vasodilator, while angiotensin receptor-1 (AT-1R) mediates vasoconstriction.
- KKS plays vital roles in preventing thrombosis and atherosclerosis and is implicated in cardiovascular diseases (CVDs) and diabetes.
Purpose of the Study:
- To highlight the essential elements of the 2015 International Kinin Symposium lecture on KKS.
- To celebrate Dr. Regoli's 60 years of research on vasoactive peptides.
- To emphasize the therapeutic significance of KKS and ACE inhibitors in managing CVDs and diabetes.
Main Methods:
- Review of lecture content from the 2015 International Kinin Symposium.
- Discussion of Dr. Regoli's research contributions.
- Analysis of the physiological roles of RAS and KKS in cardiovascular health.
Main Results:
- The B2R's vasodilatory mechanisms, including nitric oxide (NO), prostacyclin, and endothelial hyperpolarizing factor (EDHF), are essential for tissue perfusion.
- KKS's role as an autacoid on vascular endothelium is critical for cardiovascular disease prevention.
- ACE inhibitors (ACEIs) demonstrate dual action by blocking RAS and potentiating KKS.
Conclusions:
- KKS is a key regulator of cardiovascular homeostasis and a therapeutic target.
- ACE inhibitors are ideal agents for treating CVDs and diabetes due to their dual action on RAS and KKS.
- The research underscores the importance of understanding vasoactive peptide systems for disease management.
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