Interleukin 8 receptor, alpha is achemokine receptor. This name and the correspondinggene symbolIL8RA have been replaced by theHGNC approved nameC-X-C motif chemokine receptor 1 and the approved symbolCXCR1. It has also been designated asCD181 (cluster of differentiation 181). TheIUPHAR Committee on Receptor Nomenclature and Drug Classification use the HGNC recommended name, CXCR1.
The protein encoded by this gene is a member of theG-protein-coupled receptor family. This protein is a receptor forinterleukin 8 (IL8). It binds to IL8 with high affinity, and transduces the signal through a G-protein-activated second messenger system. Knockout studies in mice suggested that this protein inhibits embryonicoligodendrocyte precursor migration in developing spinal cord.IL8RA,IL8RB, which encodes another high affinity IL8 receptor, and IL8RBP, a pseudogene of IL8RB, form a gene cluster in a region mapped to chromosome 2q33-q36.[5] Stimulation of CXCR1 inneutrophils by its primary ligand,Interleukin 8, leads to neutrophilchemotaxis and activation.[6]
Blocking CXCR1 (e.g., withrepertaxin[7]) inhibits some human breast cancer stem cells (in vitro and in mice).[8]
In melanoma expression of CXCR1 at the cell surface is present, independent of the cancers stage. It is thought to have a role in the cell growth and angiogenesis required for tumour survival. In this way it has been identified as a potential therapeutic target.[9]
CXCR1 can be cleaved and inactivated by Neutrophil Derived Serine Proteases (NSPs), leading to neutrophil dysfunction and impaired bacterial killing incystic fibrosis lung disease.[10]
^Casilli F, Bianchini A, Gloaguen I, Biordi L, Alesse E, Festuccia C, et al. (February 2005). "Inhibition of interleukin-8 (CXCL8/IL-8) responses by repertaxin, a new inhibitor of the chemokine receptors CXCR1 and CXCR2".Biochemical Pharmacology.69 (3):385–394.doi:10.1016/j.bcp.2004.10.007.PMID15652230.
Ahuja SK, Ozçelik T, Milatovitch A, Francke U, Murphy PM (September 1992). "Molecular evolution of the human interleukin-8 receptor gene cluster".Nature Genetics.2 (1):31–36.doi:10.1038/ng0992-31.PMID1303245.S2CID19732372.
Morris SW, Nelson N, Valentine MB, Shapiro DN, Look AT, Kozlosky CJ, et al. (November 1992). "Assignment of the genes encoding human interleukin-8 receptor types 1 and 2 and an interleukin-8 receptor pseudogene to chromosome 2q35".Genomics.14 (3):685–691.doi:10.1016/S0888-7543(05)80169-7.PMID1427896.
Morohashi H, Miyawaki T, Nomura H, Kuno K, Murakami S, Matsushima K, et al. (January 1995). "Expression of both types of human interleukin-8 receptors on mature neutrophils, monocytes, and natural killer cells".Journal of Leukocyte Biology.57 (1):180–187.doi:10.1002/jlb.57.1.180.PMID7829970.S2CID7819367.
Schnitzel W, Monschein U, Besemer J (June 1994). "Monomer-dimer equilibria of interleukin-8 and neutrophil-activating peptide 2. Evidence for IL-8 binding as a dimer and oligomer to IL-8 receptor B".Journal of Leukocyte Biology.55 (6):763–770.doi:10.1002/jlb.55.6.763.PMID8195702.S2CID5948202.
Cerretti DP, Kozlosky CJ, Vanden Bos T, Nelson N, Gearing DP, Beckmann MP (March 1993). "Molecular characterization of receptors for human interleukin-8, GRO/melanoma growth-stimulatory activity and neutrophil activating peptide-2".Molecular Immunology.30 (4):359–367.doi:10.1016/0161-5890(93)90065-J.PMID8384312.
Mollereau C, Muscatelli F, Mattei MG, Vassart G, Parmentier M (April 1993). "The high-affinity interleukin 8 receptor gene (IL8RA) maps to the 2q33-q36 region of the human genome: cloning of a pseudogene (IL8RBP) for the low-affinity receptor".Genomics.16 (1):248–251.doi:10.1006/geno.1993.1167.PMID8486366.
Lloyd A, Modi W, Sprenger H, Cevario S, Oppenheim J, Kelvin D (1993). "Assignment of genes for interleukin-8 receptors (IL8R) A and B to human chromosome band 2q35".Cytogenetics and Cell Genetics.63 (4):238–240.doi:10.1159/000133541.PMID8500355.
"Chemokine Receptors: CXCR1".IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived fromthe original on 2016-03-03. Retrieved2008-12-03.
