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CMKLR1
Identifiers
Aliases	CMKLR1, CHEMERINR, ChemR23, DEZ, RVER1, chemerin chemokine-like receptor 1, CCX832
External IDs	OMIM: 602351; MGI: 109603; HomoloGene: 129967; GeneCards: CMKLR1; OMA:CMKLR1 - orthologs
Gene location (Human)
Chr.	Chromosome 12 (human)
End	108,339,317 bp
Gene location (Mouse)
Chr.	Chromosome 5 (mouse)
End	113,788,487 bp
RNA expression pattern
	Top expressed in
	right coronary artery; ; Descending thoracic aorta; ; Achilles tendon; ; tendon of biceps brachii; ; ascending aorta; ; granulocyte; ; spleen; ; left coronary artery; ; monocyte; ; tibial arteries;
	Top expressed in
	zygote; ; secondary oocyte; ; white adipose tissue; ; primary oocyte; ; subcutaneous adipose tissue; ; tail of embryo; ; internal carotid artery; ; mesenteric lymph nodes; ; stroma of bone marrow; ; external carotid artery;
	More reference expression data
	; ;
	More reference expression data
Gene ontology
Molecular function	G protein-coupled receptor activity; protein binding; chemokine receptor activity; signal transducer activity; signaling receptor activity;
Cellular component	integral component of membrane; integral component of plasma membrane; membrane; plasma membrane;
Biological process	chemotaxis; skeletal system development; G protein-coupled receptor signaling pathway; positive regulation of macrophage chemotaxis; negative regulation of NF-kappaB transcription factor activity; positive regulation of fat cell differentiation; immune response; regulation of calcium-mediated signaling; signal transduction; negative regulation of interleukin-12 production; chemokine-mediated signaling pathway; complement receptor mediated signaling pathway; inflammatory response; phospholipase C-activating G protein-coupled receptor signaling pathway; positive regulation of cytosolic calcium ion concentration; positive regulation of cold-induced thermogenesis;
	Sources:Amigo / QuickGO
Orthologs
	1240
	14747
	ENSG00000174600
	ENSMUSG00000042190
	Q99788
	P97468
	NM_004072; NM_001142343; NM_001142344; NM_001142345
	NM_008153; NM_001359060
	NP_001135815; NP_001135816; NP_001135817; NP_004063
	NP_032179; NP_001345989
	Wikidata
View/Edit Human	View/Edit Mouse

Chemokine like receptor 1 also known as ChemR23 (Chemerin Receptor 23) is a protein that in humans is encoded by the CMKLR1 gene.^[5]^[6] Chemokine receptor-like 1 is a G protein-coupled receptor for the chemoattractant adipokine chemerin^[7] and the omega-3 fatty acid eicosapentaenoic acid-derived specialized pro-resolving molecule, resolvin E1 (see Specialized proresolving mediators#EPA-derived resolvins (i.e. RvE)).^[8] The murine receptor that shares almost 80% homology with the human receptor, is called Dez.^[9]

Tissue distribution

CMKLR1 shows wide RNA expression profile but is notably high in plasmacytoid dendritic cells, macrophages, cardiomyocytes, adipocytes and endothelial cells.^[10]

Function

Activating CMKLR1 by an agonist mobilizes intracellular calcium and causes the activation of several other signaling cascades like the ERK1 and NF-κB. Initial studies of CMKLR1 suggested that it might have a role in the inflammatory pathways. Its cognate ligand, chemerin was found in joint aspirate from rheumatoid arthritis and absent in aspirate from degenerative arthritis. CMKLR1 expression by plasmacytoid dendritic cells and macrophages also helped foster this idea. In vitro chemotaxis assays showed it to be utilized in attracting these cells. As an adipokine receptor it has a role in adipogenesis and adipocyte maturation.^[11] It seems also to have a role in peripheral insulin resistance.^[12]

Also studies using the mouse zymosan model and chemerin peptides showed that these peptides suppressed and helped resolve the peritonitis in mice.^[13] The same model showed that this particular molecule enhances macrophage efferocytosis (phagocyting apoptotic cells).^[14]

Receptor antagonist CCX832

CCX832 is an orally active molecule used as a tool compound in experimental pharmacology. It antagonises the effect of CMKLR1.^[15]^[16]^[17] It is listed on the Guide to Pharmacology database as the only example of a CMKLR1 antagonist. Its chemical structure is undisclosed.^[18]

The substance was originally developed for use as a pharmaceutical drug against inflammatory diseases by ChemoCentryx, a pharmaceutical firm based in California, in alliance with GlaxoSmithKline (GSK).^[19] Development was terminated after a Phase I clinical trial in 2012.^[20]