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Formylpeptide receptors: A novel target to treat cardiometabolic complications
Chen Huei Leo1, Elizabeth A Vecchio2, Ting Fu2
1Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Melbourne, VIC, Australia; Department of Biomedical Engineering, College of Design and Engineering, National University of Singapore, Singapore 117576, Singapore.
Abstract:
The formylpeptide receptor (FPR) family, particularly FPR2, has emerged as a master regulator of inflammation and its resolution. Given that both cardiovascular diseases and metabolic disorders are characterised by pro-inflammatory scenarios, often with resultant impairment of the healing response to (i.e. resolution of) inflammation, therapeutic targeting of the FPR family with judicious agonist selection provides new promise for tackling cardiometabolic disease. Here, we consider the pharmacology of this intriguing receptor family, the potential for novel biased signalling at its receptor subtypes and the current status of both endogenous and synthetic agonists (including peptides/proteins, small molecules and lipids) reported to be active at FPRs. A detailed review of the therapeutic potential of published FPR ligands involved in regulating and resolving inflammation in cardiometabolic disease is also provided. We anticipate that a broader understanding of, and greater appreciation for, the translational potential of pro-resolution FPR-based therapies may offer new effective means of targeting a range of cardiometabolic disorders and their resultant complications.
Insights
Targeting formylpeptide receptors (FPRs), especially FPR2, offers new hope for treating inflammation in cardiometabolic diseases. Therapies modulating FPRs may resolve inflammation, improving outcomes for cardiovascular and metabolic disorders.
Area of Science:
- Immunology
- Pharmacology
- Cardiovascular Science
Background:
- Cardiovascular diseases and metabolic disorders share pro-inflammatory characteristics.
- Impaired resolution of inflammation contributes to disease progression and complications.
- The formylpeptide receptor (FPR) family, particularly FPR2, plays a key role in inflammation regulation.
Purpose of the Study:
- To review the pharmacology of FPRs and their role in cardiometabolic disease.
- To explore the potential of biased signaling and novel agonists for FPRs.
- To assess the therapeutic potential of FPR ligands for treating inflammation in cardiometabolic conditions.
Main Methods:
- Literature review of published research on FPRs and their ligands.
- Analysis of endogenous and synthetic agonists targeting FPRs.
- Evaluation of FPR ligand activity in regulating and resolving inflammation.
Main Results:
- FPRs are crucial regulators of inflammation and its resolution.
- Various FPR agonists (peptides, small molecules, lipids) have been identified.
- Biased signaling at FPR subtypes offers therapeutic opportunities.
Conclusions:
- Targeting FPRs with specific agonists presents a promising therapeutic strategy for cardiometabolic diseases.
- Developing FPR-based therapies could provide novel treatments for inflammation-related complications.
- Further understanding of FPR pharmacology can advance treatment for cardiovascular and metabolic disorders.
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