CMKLR1
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| Location (UCSC) | Chr 12: 108.29 – 108.34 Mb | Chr 5: 113.75 – 113.79 Mb | |||||||
| PubMed search | [3] | [4] | |||||||
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Chemokine like receptor 1 also known as ChemR23 (Chemerin Receptor 23) is a
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
Receptor antagonist CCX832
CCX832 is an
The substance was originally developed for use as a pharmaceutical drug against
References
- ^ a b c GRCh38: Ensembl release 89: ENSG00000174600 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000042190 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Entrez Gene: CMKLR1 chemokine-like receptor 1".
- PMID 8976386.
- PMID 14530373.
- PMID 15753205.
- PMID 9144535.
- PMID 20044979.
- PMID 17635925.
- S2CID 41312338.
- PMID 18391062.
- PMID 20363975.
- PMID 28029186.
- PMID 27742615.
- PMID 27371688.
- ^ "Chemerin receptor – IUPHAR/BPS Guide to Pharmacology". www.guidetopharmacology.org. Retrieved 7 April 2017.
- ^ "ChemoCentryx Identifies Novel Small Molecule ChemR23 Antagonist for the Treatment of Inflammatory Diseases". ChemoCentryx. 2010-04-10. Archived from the original on 2011-05-19. Retrieved 2017-04-14.
- ^ "ChemoCentryx, GSK discontinue ChemR23 antagonist". BioCentury. 7 February 2012.
External links
- Human CMKLR1 genome location and CMKLR1 gene details page in the UCSC Genome Browser.
Further reading
- Owman C, Lolait SJ, Santén S, Olde B (December 1997). "Molecular cloning and tissue distribution of cDNA encoding a novel chemoattractant-like receptor". Biochemical and Biophysical Research Communications. 241 (2): 390–4. PMID 9425281.
- Samson M, Edinger AL, Stordeur P, Rucker J, Verhasselt V, Sharron M, Govaerts C, Mollereau C, Vassart G, Doms RW, Parmentier M (May 1998). "ChemR23, a putative chemoattractant receptor, is expressed in monocyte-derived dendritic cells and macrophages and is a coreceptor for SIV and some primary HIV-1 strains". European Journal of Immunology. 28 (5): 1689–700. PMID 9603476.
- Hillman RT, Green RE, Brenner SE (2005). "An unappreciated role for RNA surveillance". Genome Biology. 5 (2): R8. PMID 14759258.
- Mårtensson UE, Fenyö EM, Olde B, Owman C (November 2006). "Characterization of the human chemerin receptor--ChemR23/CMKLR1--as co-receptor for human and simian immunodeficiency virus infection, and identification of virus-binding receptor domains". Virology. 355 (1): 6–17. PMID 16904155.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.