Target intelligence / Profile preview

Chemerin receptor 1 (CMKLR1)

Target
CMKLR1
Molecular classification
G protein-coupled receptor, Receptor, Chemoattractant receptor, Class A GPCR (γ-subgroup)
01

Overview

Chemerin receptor 1 (CMKLR1, also known as ChemR23 or Chemerin receptor 23) is a chemoattractant G protein-coupled receptor (GPCR) predominantly expressed on innate immune cells such as macrophages, dendritic cells, and neutrophils. Its primary endogenous ligands are chemerin, an adipokine involved in chemotaxis and inflammatory regulation, and Resolvin E1 (RvE1), a specialized pro-resolving lipid mediator derived from eicosapentaenoic acid. Activation of ChemR23 modulates immune cell migration, promotes the clearance of apoptotic cells (efferocytosis), and reprograms macrophages toward anti-inflammatory and pro-resolving phenotypes, which are processes implicated in the resolution of inflammation, tissue repair, metabolic regulation, and suppression of pathological immune responses. The receptor is recognized as a promising therapeutic target in chronic inflammatory diseases, obesity, cancer, cardiovascular disease, and neurodegenerative conditions, with several agonists and antagonists in preclinical and early clinical studies.

Other names
ChemR23Chemokine-like receptor 1Chemerin receptor 23Chemerin receptorG protein-coupled receptor DEZGPR1 (sometimes refers to a related but distinct receptor)
02

Mechanism of action

Agonists (e.g., Resolvin E1, chemerin-derived peptides, agonist antibodies) promote anti-inflammatory or pro-resolving macrophage functions and enhance efferocytosis Antagonists (e.g., CCX832) block receptor’s pro-inflammatory signaling

03

Biological functions

Signal transductionChemotaxis of macrophages and dendritic cellsRegulation of inflammation (pro- and anti-inflammatory effects)Resolution of inflammationAdipogenesis and adipocyte maturationRegulation of metabolic processesPromotion of macrophage efferocytosis (clearance of apoptotic cells)
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Disease associations

InflammationCancerCardiovascular diseaseObesity/metabolic syndromeNeurodegenerative diseaseInfection
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Safety considerations

Modulation of immune functions may carry risk of immune suppression or impaired host defenseTargeting resolution of inflammation pathways may affect normal tissue repair and defense mechanismsClinical safety profile still being established for investigational drugs
06

Interacting drugs

Resolvin E1 (RvE1) (endogenous lipid mediator agonist)

2 more in the full profile.

07

Biomarkers

CMKLR1 (ChemR23) expression on tumor-associated macrophages and innate immune cells (e.g., in breast cancer, mesothelioma, colon inflammation)Circulating chemerin levels (indirectly related)

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