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CXCR1

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 68

Nomenclature: CXCR1

Family: Chemokine receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 350 2q35 CXCR1 C-X-C motif chemokine receptor 1 28,35
Mouse 7 351 1 38.44 cM Cxcr1 C-X-C motif chemokine receptor 1 19
Rat 7 349 9q33 Cxcr1 C-X-C motif chemokine receptor 1 11
Previous and Unofficial Names Click here for help
IL8RA [35] | IL-8 receptor type I | CD181 | CKR-1 | CXC-R1 | high affinity interleukin-8 receptor A | CXCR1-like [11] | IL-8 receptor α
Database Links Click here for help
Specialist databases
GPCRdb cxcr1_human (Hs), cxcr1_mouse (Mm), cxcr1_rat (Rn)
Other databases
Alphafold P25024 (Hs), Q810W6 (Mm), P70612 (Rn)
ChEMBL Target CHEMBL4029 (Hs)
Ensembl Gene ENSG00000163464 (Hs), ENSMUSG00000048480 (Mm), ENSRNOG00000048239 (Rn)
Entrez Gene 3577 (Hs), 227288 (Mm), 54258 (Rn)
Human Protein Atlas ENSG00000163464 (Hs)
KEGG Gene hsa:3577 (Hs), mmu:227288 (Mm), rno:54258 (Rn)
OMIM 609423 (Hs), 146929 (Hs)
Pharos P25024 (Hs)
RefSeq Nucleotide NM_000634 (Hs), NM_178241 (Mm), NM_019310 (Rn)
RefSeq Protein NP_000625 (Hs), NP_839972 (Mm), NP_062183 (Rn)
UniProtKB P25024 (Hs), Q810W6 (Mm), P70612 (Rn)
Wikipedia CXCR1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of human CXCR1 in phospholipid bilayers
PDB Id:  2LNL
Resolution:  0.0Å
Species:  Human
References:  46
Natural/Endogenous Ligands Click here for help
CXCL6 {Sp: Human}
CXCL8 {Sp: Human}
cytokine domain of tyrosyl tRNA synthetase {Sp: Human}
Comments: CXCL8 is the principal endogenous agonist

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]CXCL8 (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.9 – 9.6 pKd 26,49
⤷ pKd 8.9 – 9.6 (Kd 1.2x10-9 – 2.51x10-10 M) [26,49]
CXCL8 {Sp: Human} Peptide Click here for species-specific activity table Immunopharmacology Ligand Hs Agonist 8.1 pKd 23
⤷ pKd 8.1 (Kd 8x10-9 M) [23]
[125I]mini-TyrRS Peptide Ligand is labelled Ligand is radioactive Hs Full agonist 7.7 pKd 54
⤷ pKd 7.7 [54]
CXCL8 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.8 – 9.5 pKi 3,26,35,56,58
⤷ pKi 8.8 – 9.5 [3,26,35,56,58]
mini-TyrRS Peptide Hs Full agonist 8.1 pKi 54
⤷ pKi 8.1 [54]
CXCL6 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.0 pKi 59
⤷ pKi 7.0 [59]
vCXCL1 Peptide Click here for species-specific activity table Hs Agonist 7.4 pIC50 39
⤷ pIC50 7.4 (IC50 4.4x10-8 M) [39]
Agonist Comments
Reference [48] measures agonist potency using a MAP kinase reporter gene.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
navarixin Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 8.4 pIC50 2,12
⤷ pIC50 8.4 (IC50 3.9x10-9 M) [2,12]
AZD5069 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.9 pIC50 43
⤷ pIC50 6.9 (IC50 1.25x10-7 M) [43]
Description: Measuring displacement of CXCL8 binding to recombinant CXCR1 in HEK cell membrane preparations.
Allosteric Modulator Comments
DF2755A and DF2726 are non-competitive negative allosteric modulators of CXCL8 signalling via CXCR1 and CXCR2 [4,38].
Immunopharmacology Comments
CXCR1 is one of more than 20 distinct chemokine receptors expressed in human leukocytes. Chemokines primarily act to promote leukocyte chemotaxis to sites of inflammation. CXCR1 is discussed in relation to immuno-oncology in [1]. It has been shown that CXCR1 receptor expression on epithelial cells is enhanced by bacterial infection (E.coli [24,27] and H. pylori[6]). This induces transepithelial neutrophil migration and clearing of the infection.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
Calcium channel
Comments:  The βγ subunit of the Gi G protein is necessary for chemotaxis [42] and calcium mobilisation [26].
References:  16,26,42
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Calcium channel
Phospholipase D stimulation
Other - See Comments
Comments:  Superoxide production is also reported [55]. Additional information on signaling pathways can be found in [33]. Agonists at high concentrations induce phosphorylation of CXCR1, leading to homologous desensitization and receptor internalization [15]. CXCR1 couples to G-protein-coupled receptor kinase 2 (GRK2, gene symbol ADRBK1) to negatively regulate receptor sensitization and trafficking [47].
References:  26,33
Tissue Distribution Click here for help
NK cells and lymphocytes.
Species:  Human
Technique:  FACS
References: 
Effector CD8+ T cells.
Species:  Human
Technique:  FACS
References:  52
Keratinocytes.
Species:  Human
Technique:  Radioligand binding.
References:  41
Primary adult microglia and astrocytes.
Species:  Human
Technique:  Flow cytometry.
References:  17
Polymorphonuclear neutrophils.
Species:  Human
Technique:  Flow cytometry.
References:  10
Intestinal epithelial cells.
Species:  Human
Technique:  RT-PCR and flow cytometry.
References:  51
Bronchial epithelial cells.
Species:  Human
Technique:  RT-PCR and flow cytometry.
References:  14
Urinary tract epithelial cells.
Species:  Human
Technique:  Immunohistochemistry.
References:  24
Chondrocytes.
Species:  Human
Technique:  Flow cytometry.
References:  40
D4+ FOXP3+ Tregs (regulatory T cells).
Species:  Human
Technique:  FACS
References:  13
Umbilical vein endothelial cells (HUVECs).
Species:  Human
Technique:  immunocytochemistry.
References:  36
Basophils.
Species:  Human
Technique:  Flow cytometry.
References:  30,44
Basophils.
Species:  Human
Technique:  RT-PCR.
References:  30
Glomerular podocytes.
Species:  Human
Technique:  RT-PCR.
References:  29
CX3CR1low CD14+ monocytes.
Species:  Human
Technique:  FACS
References:  20
Lung, spleen.
Species:  Mouse
Technique:  Northern blotting.
References:  19
Peripheral blood leukocytes, isolated neutrophils > thymus, peritoneal monocytes/macrophages.
Species:  Mouse
Technique:  RT-PCR.
References:  19
Lung and native macrophages.
Species:  Rat
Technique:  Northern blotting.
References:  11
Tissue Distribution Comments
CXCR1 is also expressed by many non-hematopoietic cells, including tumor cells.
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of intracellular Ca2+ levels in HEK 293 cells transfected with the human CXCR1 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in intracellular Ca2+.
References:  35,59-60
Measurement of chemotaxis in of HEK 293 cells transfected with the CXCR1 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Chemotaxis.
References:  16,42,59
Measurement of Ca2+ levels in Jurkat cells transfected with the human CXCR1 receptor.
Species:  Human
Tissue:  Jurkat cells.
Response measured:  Ca2+ mobilisation.
References:  32-33,57
Measurement of elastase released by human neutrophils endogenously expressing the CXCR1 receptor.
Species:  Human
Tissue:  Neutrophils.
Response measured:  Release of elastase.
References:  32-33,57
Measurement of superoxide production (indicating respiratory burst) in human neutrophils endogenously expressing the CXCR1 receptor.
Species:  Human
Tissue:  Neutrophils.
Response measured:  Superoxide production.
References:  32-33
Measurement of phospholipase D (PLD) activity in human neutrophils endogenously expressing the CXCR1 receptor.
Species:  Human
Tissue:  Neutrophils.
Response measured:  Activation of PLD.
References:  33
Measurement of focal adhesion kinase (FAK) activity and chemotaxis of HEK 293 and RBL cells transfected with the CXCR1 receptor.
Species:  Human
Tissue:  HEK 293 and RBL cells.
Response measured:  FAK phosphorylation.
References:  16
Measurement of chemotaxis of Jurkat cells transfected with the human CXCR1 receptor.
Species:  Human
Tissue:  Jurkat cells.
Response measured:  Chemotaxis.
References:  25,57
Measurement of cAMP levels in CHO cells transfected with the human CXCR1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Inhibition of cAMP accumulation.
References:  26
Phosphorylation of focal adhesion kinase.
Species:  Human
Tissue:  Human CXCR1-transfected RBL 2H3 cells.
Response measured:  Elevated spreading.
References:  9
Physiological Functions Click here for help
Chemotaxis.
Species:  Human
Tissue:  Keratinocytes.
References:  41
Chemotaxis.
Species:  Human
Tissue:  Intestinal epithelial cells.
References:  51
Chemotaxis across the epithelial barrier of the urinary tract.
Species:  Human
Tissue:  Neutrophils.
References:  24
Cell proliferation and inhibition of apoptosis.
Species:  Human
Tissue:  Umbilical vein endothelial cells (HUVECs).
References:  36
Negative regulation of myeloid progenitor cells.
Species:  Mouse
Tissue:  In vivo.
References:  5
Promoting allergic disease.
Species:  Human
Tissue:  CXCR1+CD4+ T cells.
References:  18
Proliferation of endothelial cells.
Species:  Human
Tissue:  HUVEC and HMEC cells.
References:  37
Physiological Functions Comments
CXCR1 is implicated in directed intravascular leukocyte migration through platelet thrombi at sites of vascular injury [21]. CXCR1 is also implicated as a negative determinant for pancreatic islet survival after transplantation [8].
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Cxcr1tm1Dgen Cxcr1tm1Dgen/Cxcr1tm1Dgen
involves: 129P2/OlaHsd * C57BL/6		 MGI:2448715  MP:0002169 no abnormal phenotype detected
Clinically-Relevant Mutations and Pathophysiology Comments
Administration of reparixin in on-pump coronary artery bypass grafting (CABG) patients appears to be feasible and safe. It concurrently attenuated postoperative granulocytosis in peripheral blood [45].
In many malignancies, elevated CXCR1 activity has been connected to increased tumor growth and metastasis.
Biologically Significant Variants Click here for help
Type:  Missense mutation
Species:  Human
Description:  This single nucleotide polymorphism causes a missense variant which is associated with significantly increased susceptibility to acute pyelonephritis in childhood.
Amino acid change:  Ser276Thr
Nucleotide change:  827G>C
Global MAF (%):  14
Subpopulation MAF (%):  AFR|AMR|ASN|EUR: 26|9|9|4
Minor allele count:  G=0.115/250
SNP accession:  rs2234671
References:  31
Type:  Missense mutation
Species:  Human
Description:  Met to Arg variant in the N terminus extracellular domain of CXCR1. This mutation reduces infection by HIV, probably acting through modulation of CD4 and CXCR4 expression.
Amino acid change:  Met31Arg
Global MAF (%):  4
SNP accession:  rs16858811
References:  22,53
Type:  Single nucleotide polymorphism
Species:  Human
Description:  This single nucleotide polymorphism is associated with susceptibility to cutaneous leishmaniasis.
Nucleotide change:  C>G
Global MAF (%):  18
SNP accession:  rs2854386
References:  7
Type:  Single nucleotide polymorphisms
Species:  Human
Description:  Multiple CXCR1 single nucleotide variants are associated with cystic fibrosis.
References:  34
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  Ser342Leu
Global MAF (%):  1
Subpopulation MAF (%):  AFR: 5
Minor allele count:  A=0.012/26
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession:  VAR_021062, rs16858806
Validation:  1000 Genomes, HapMap
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  Met268Leu
Global MAF (%):  1
Subpopulation MAF (%):  AFR: 2
Minor allele count:  G=0.006/13
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession:  VAR_026525, rs9282752
Validation:  HapMap, Frequency, Multiple observations
Type:  Single nucleotide polymorphism
Species:  Human
Description:  This single nucleotide polymorphism may be associated with an increased risk of developing chronic obstructive pulmonary disease and asthma.
Amino acid change:  Arg335Cys
Nucleotide change:  1122C>T
Minor allele count:  A=0.0230/115
Comment on frequency:  Low frequency of expression (<10% in all tested populations)
SNP accession:  rs16858808
References:  50

References

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