Target intelligence / Profile preview

Resolvin receptor

Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Resolvin receptors are a family of G protein-coupled receptors (GPCRs) that mediate the biological actions of resolvins, which are specialized pro-resolving mediators (SPMs) derived from omega-3 polyunsaturated fatty acids like EPA and DHA (Serhan et al., 2002). The most well-characterized members include the Resolvin E1 receptor (CMKLR1 or ChemR23) and the Resolvin D1 receptors (FPR2/ALX and GPR32) (Chiang et al., 2012). These receptors are primarily expressed on leukocytes, including neutrophils and macrophages, where they signal to actively terminate the inflammatory response. Upon activation, they inhibit further neutrophil recruitment, promote the non-phlogistic recruitment of monocytes, and stimulate the phagocytosis of apoptotic cells and microbes to clear cellular debris (Serhan, 2014). Because they promote the active resolution of inflammation rather than simply blocking inflammatory pathways, these receptors are attractive therapeutic targets for chronic inflammatory diseases such as asthma, rheumatoid arthritis, and atherosclerosis (Dalli et al., 2013). Several resolvin analogs and small-molecule agonists are currently being investigated in clinical and preclinical studies for their potential to treat inflammatory conditions without the immunosuppressive side effects associated with traditional anti-inflammatory drugs.

Other names
Specialized pro-resolving mediator receptorSPM receptorN-formyl peptide receptor 2 (FPR2)ALX/FPR2Chemerin chemokine-like receptor 1 (CMKLR1)ChemR23G protein-coupled receptor 32 (GPR32)G protein-coupled receptor 18 (GPR18)ERV1DRV1DRV2
02

Mechanism of action

Agonism of specific G protein-coupled receptors to activate pro-resolving signaling pathways that limit neutrophil infiltration and enhance macrophage-mediated clearance of apoptotic cells.

03

Biological functions

Immune responseResolution of inflammationSignal transductionPhagocytosisApoptosis
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Disease associations

InflammationCardiovascular diseaseAsthmaArthritisInfectionNeurodegenerative disease
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Safety considerations

Potential for impaired host defense if resolution is over-stimulatedOff-target GPCR activationLipid stability and bioavailability challenges
06

Interacting drugs

Resolvin E1 (RX-10001)

5 more in the full profile.

07

Biomarkers

High-sensitivity C-reactive protein (hsCRP)Pro-inflammatory cytokine levels (IL-6, TNF-alpha)Lipid mediator profiles (LC-MS/MS)Neutrophil-to-lymphocyte ratio

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