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CXCR3

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 70

Nomenclature: CXCR3

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 7 368 Xq13.1 CXCR3 C-X-C motif chemokine receptor 3 18
Mouse 7 367 X 44.58 cM Cxcr3 C-X-C motif chemokine receptor 3 26
Rat 7 367 Xq22 Cxcr3 C-X-C motif chemokine receptor 3 29
Previous and Unofficial Names Click here for help
GPR9 | CD183 | MigR | G protein-coupled receptor 9 | IP-10 receptor | CXC-R3 | interferon-inducible protein 10 receptor | Cxcr3 | CKR-L2 | chemokine (C-X-C motif) receptor 3
Database Links Click here for help
Specialist databases
GPCRdb cxcr3_human (Hs), cxcr3_mouse (Mm), cxcr3_rat (Rn)
Other databases
Alphafold P49682 (Hs), O88410 (Mm), Q9JII9 (Rn)
ChEMBL Target CHEMBL4441 (Hs), CHEMBL5200 (Mm), CHEMBL1075172 (Rn)
Ensembl Gene ENSG00000186810 (Hs), ENSMUSG00000050232 (Mm), ENSRNOG00000003305 (Rn)
Entrez Gene 2833 (Hs), 12766 (Mm), 84475 (Rn)
Human Protein Atlas ENSG00000186810 (Hs)
KEGG Gene hsa:2833 (Hs), mmu:12766 (Mm), rno:84475 (Rn)
OMIM 600894 (Hs)
Pharos P49682 (Hs)
RefSeq Nucleotide NM_001504 (Hs), NM_009910 (Mm), NM_053415 (Rn)
RefSeq Protein NP_001495 (Hs), NP_034040 (Mm), NP_445867 (Rn)
UniProtKB P49682 (Hs), O88410 (Mm), Q9JII9 (Rn)
Wikipedia CXCR3 (Hs)
Natural/Endogenous Ligands Click here for help
CCL5 {Sp: Human}
CCL7 {Sp: Human}
CCL11 {Sp: Human}
CCL13 {Sp: Human}
CCL20 {Sp: Human}
CCL19 {Sp: Human}
CXCL12α {Sp: Human}
CXCL10 {Sp: Human}
CXCL11 {Sp: Human}
CXCL9 {Sp: Human} , CXCL9 {Sp: Mouse}
CXCL10 {Sp: Mouse}
CXCL11 {Sp: Mouse}
CXCL10 {Sp: Rat}

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
CXCL11 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 10.4 – 10.5 pKi 8
⤷ pKi 10.4 – 10.5 [8]
CXCL10 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.8 – 9.8 pKi 8,30
⤷ pKi 7.8 – 9.8 [8,30]
CXCL9 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.3 – 8.3 pKi 8,30
⤷ pKi 7.3 – 8.3 [8,30]
CCL13 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.2 pKi 30
⤷ pKi 7.2 [30]
CCL20 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 6.8 pKi 30
⤷ pKi 6.8 [30]
CCL5 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 6.4 pKi 30
⤷ pKi 6.4 [30]
CXCL12α {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 6.4 pKi 30
⤷ pKi 6.4 [30]
CCL19 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 5.9 pKi 30
⤷ pKi 5.9 [30]
Agonist Comments
It has been reported that CCL11, despite binding with high affinity, may be neither an agonist or an antagonist of the CXCR3 receptor, but sequesters available CCL11 resulting in a lowered response at other receptors [32].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ACT-777991 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 8.3 pKd 19
⤷ pKd 8.3 (Kd 4.6x10-9 M) [19]
Description: Binding affinity determined in an association assay using [3H]ACT-777991
NBI-74330 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 8.3 – 8.8 pKi 8
⤷ pKi 8.3 – 8.8 [8]
CCL11 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Antagonist 7.2 pKi 30
⤷ pKi 7.2 [30]
CCL7 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Antagonist 6.6 pKi 30
⤷ pKi 6.6 [30]
ACT-660602 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 8.6 pIC50 20
⤷ pIC50 8.6 (IC50 2.7x10-9 M) [20]
Description: Antagonist potency determined by FLIPR calcium mobilization assay, in CHO-K1 cells expressing recombinant CXCR3 receptors with CXCL10 as agonist
ACT-777991 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 8.5 pIC50 19
⤷ pIC50 8.5 (IC50 3.3x10-9 M) [19]
Description: Antagonism of CXCL9-mediated CXCR3 activation in a calcium signaling assay
AMG487 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 8.1 pIC50 11
⤷ pIC50 8.1 (IC50 8x10-9 M) [11]
Description: Antagonism of 125I-IP10 binding to CXCR3 in a radioligand competition binding assay
duramycin Peptide Hs Antagonist 7.0 pIC50 22
⤷ pIC50 7.0 [22]
dioscin Small molecule or natural product Hs Antagonist 6.3 pIC50 22
⤷ pIC50 6.3 [22]
hypoglaucin A Small molecule or natural product Hs Antagonist 5.7 pIC50 22
⤷ pIC50 5.7 [22]
kallstroemin D Small molecule or natural product Hs Antagonist 5.5 pIC50 22
⤷ pIC50 5.5 [22]
Immunopharmacology Comments
CXCR3 is one of more than 20 distinct chemokine receptors expressed in human leukocytes. Chemokines primarily act to promote leukocyte chemotaxis to sites of inflammation. CXCR3 is the receptor for CXCL9, -10 and -11, three CXC chemokines that are preferentially expressed on Th1 lymphocytes.

In the cancer setting cytokines are known to establish an immunosuppressive milieu that is condusive to tumour progression. CXCR3 and its ligands have specifically been identified as being associated with this mechanism in pancreatic ductal adenocarcinoma [3].
Cell Type Associations
Immuno Cell Type:  T cells
Cell Ontology Term:   T-helper 1 cell (CL:0000545)
References:  18,25
Immuno Cell Type:  Dendritic cells
Comment:  N.B. inflammatory dentritic cells
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   macrophage (CL:0000235)
Immuno Cell Type:  B cells
Cell Ontology Term:   B cell (CL:0000236)
Immuno Cell Type:  Natural killer cells
Cell Ontology Term:   natural killer cell (CL:0000623)
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Calcium channel
References:  6,15,18,29
Tissue Distribution Click here for help
Glomerular podocytes.
Species:  Human
Technique:  RT-PCR.
References:  9
T lymophocytes.
Species:  Human
Technique:  Flow cytometry.
References:  17
CD4+ T lymphocytes.
Species:  Human
Technique:  Flow cytometry.
References:  13
Osteoblasts.
Species:  Human
Technique:  RT-PCR and flow cytometry.
References:  16
B cells.
Species:  Human
Technique:  Flow cytometry.
References:  27
Primary adult microglia and astrocytes.
Species:  Human
Technique:  Flow cytometry.
References:  7
Th1-type lymphocytes.
Species:  Human
Technique:  RT-PCR.
References:  21
Tracheocytes.
Species:  Human
Technique:  immunocytochemistry.
References:  12
Lung mast cells (HLMCs).
Species:  Human
Technique:  Flow cytometry and immunofluorescence.
References:  2
Peripheral blood T lymphocytes.
Species:  Human
Technique:  RT-PCR.
References:  15
Intestinal myofibroblasts.
Species:  Human
Technique:  RT-PCR.
References:  14
T cells, B cells and natural killer cells.
Species:  Human
Technique:  Three color immunofluorescence.
References:  23
Differential expression of CXCR3-A and CXCR3-B on subsets of endothelial cells.
Species:  Human
Technique:  Immunohistochemistry.
References:  15
Eosinophils.
Species:  Human
Technique:  Flow cytometry, immunocytochemistry and RT-PCR.
References:  10
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 chemotaxis of microglia endogenously expressing the CXCR3 receptor.
Species:  Mouse
Tissue:  Microglia.
Response measured:  Chemotaxis.
References:  24
Measurement of Ca2+ levels in mouse pre-B cells transfected with the CXCR3 receptor.
Species:  Human
Tissue:  Mouse pre-B cells, 300-19.
Response measured:  Ca2+ mobilisation.
References:  18
Measurement of chemotaxis in mouse pre-B cells transfected with the CXCR3 receptor.
Species:  Human
Tissue:  Mouse pre-B cells, 300-19.
Response measured:  Chemotaxis.
References:  18
Measurement of Ca2+ levels in HEK 293 cells transfected with the mouse CXCR3 receptors.
Species:  Mouse
Tissue:  HEK 293 cells.
Response measured:  Ca2+ mobilisation.
References:  26
Measurement if Ca2+ levels in HEK 293 cells transfected with the rat CXCR3 receptor.
Species:  Rat
Tissue:  HEK 293 cells.
Response measured:  Ca2+ mobilisation.
References:  29
Measurement if Ca2+ levels in HEK 293 cells transfected with the human CXCR3 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Ca2+ mobilisation.
References:  29
Measurement of Cl- conductance in microglia endogenously expressing the CXCR3 receptor.
Species:  Mouse
Tissue:  Microglia.
Response measured:  Stimulation of a Cl- current.
References:  24
Measurement of cell proliferation and 3H-thymidine incorporation in human bronchial epithelial cells endogenously expressing the CXCR3 receptor.
Species:  Human
Tissue:  Bronchial epithelial cells.
Response measured:  Cell proliferation and 3H-thymidine incorporation.
References:  1
Measurement of MAPK pathway activity in human bronchial epithelial cells endogenously expressing the CXCR3 receptor.
Species:  Human
Tissue:  Bronchial epithelial cells.
Response measured:  ERK1/2 and p38 phosphorylation.
References:  1
Measurement of PKB activity in intestinal myofibroblasts endogenously expressing the CXCR3 receptor.
Species:  Human
Tissue:  Intestinal myofibroblasts.
Response measured:  PI3K-dependent PKB phosphorylation.
References:  14
Measurement of MAPK pathway activity in intestinal myofibroblasts endogenously expressing the CXCR3 receptor.
Species:  Human
Tissue:  Intestinal myofibroblasts.
Response measured:  ERK1/2 and p90RSK phosphorylation.
References:  14
Physiological Functions Click here for help
Chemotaxis.
Species:  Mouse
Tissue:  Microglia.
References:  24
Leukocyte recruitment.
Species:  Mouse
Tissue:  In vivo.
References:  5,28
Neovascularisation (angiogenesis).
Species:  Mouse
Tissue:  In vivo.
References:  28
Physiological Consequences of Altering Gene Expression Click here for help
CXCR3 receptor knockout mice exhibit impaired neovascular (angiogenic) response.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  28
Following bacterial inoculation of the lung, CXCR3 receptor knockout mice exhibit decreased lymphocyte and NK cell recruitment as well as delayed clearence of bacteria.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  31
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
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0009858 abnormal cellular extravasation PMID: 15152045  15718500 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Y
B6.Cg-Cxcr3		 MGI:1277207  MP:0009858 abnormal cellular extravasation PMID: 15718500 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0008750 abnormal interferon level PMID: 15254596 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Y
B6.Cg-Cxcr3		 MGI:1277207  MP:0008750 abnormal interferon level PMID: 15254596 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0003710 abnormal physiological neovascularization PMID: 15718500 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Y
B6.Cg-Cxcr3		 MGI:1277207  MP:0003710 abnormal physiological neovascularization PMID: 15718500 
Cxcr3tm1Raks Cxcr3tm1Raks/Cxcr3tm1Raks
B6.129P2-Cxcr3		 MGI:1277207  MP:0002871 albuminuria PMID: 19734217 
Cxcr3tm1Raks Cxcr3tm1Raks/Cxcr3tm1Raks
B6.129P2-Cxcr3		 MGI:1277207  MP:0005566 decreased blood urea nitrogen level PMID: 19734217 
Cxcr3tm1Raks Cxcr3tm1Raks/Cxcr3tm1Raks
B6.129P2-Cxcr3		 MGI:1277207  MP:0005554 decreased circulating creatinine level PMID: 19734217 
Cxcr3tm1Raks Cxcr3tm1Raks/Cxcr3tm1Raks
B6.129P2-Cxcr3		 MGI:1277207  MP:0005166 decreased susceptibility to injury PMID: 19734217 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0002410 decreased susceptibility to viral infection PMID: 15152045 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0009790 decreased susceptibility to viral infection induced morbidity/mortality PMID: 15152045 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0003045 fibrosis PMID: 15254596 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Y
B6.Cg-Cxcr3		 MGI:1277207  MP:0003045 fibrosis PMID: 15254596 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0005496 impaired macrophage recruitment PMID: 15718500 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Y
B6.Cg-Cxcr3		 MGI:1277207  MP:0005496 impaired macrophage recruitment PMID: 15718500 
Cxcr3tm1Dgen Cxcr3tm1Dgen/Y
involves: 129P2/OlaHsd * C57BL/6		 MGI:1277207  MP:0005559 increased circulating glucose level
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0004751 increased length of allograft survival PMID: 11085753 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Y
B6.Cg-Cxcr3		 MGI:1277207  MP:0004751 increased length of allograft survival PMID: 11085753 
Cxcr3tm1Wwh|Tg(TRAMP)8247Ng Cxcr3tm1Wwh/Cxcr3tm1Wwh,Tg(TRAMP)8247Ng/?
involves: C57BL/6		 MGI:1277207  MGI:2680364  MP:0003721 increased tumor growth/size PMID: 16941672 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
Not Specified		 MGI:1277207  MP:0002020 increased tumor incidence PMID: 20713880 
Cxcr3tm1Raks Cxcr3tm1Raks/Cxcr3tm1Raks
B6.129P2-Cxcr3		 MGI:1277207  MP:0001859 kidney inflammation PMID: 19734217 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0001861 lung inflammation PMID: 15254596 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Y
B6.Cg-Cxcr3		 MGI:1277207  MP:0001861 lung inflammation PMID: 15254596 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Cxcr3tm1Wwh
B6.Cg-Cxcr3		 MGI:1277207  MP:0003426 pulmonary interstitial fibrosis PMID: 15254596 
Cxcr3tm1Wwh Cxcr3tm1Wwh/Y
B6.Cg-Cxcr3		 MGI:1277207  MP:0003426 pulmonary interstitial fibrosis PMID: 15254596 
Biologically Significant Variants Click here for help
Type:  Splice variant
Species:  Human
Description:  CXCR3-B is a splice variant of the CXCR3 (or CXCR3-A) receptor and has been found in human airway epithelial cells.
References:  1,12,15
Type:  Single nucleotide polymorphism
Species:  Human
Description:  A polymorphism in intron 1, c.12+234G > A, may be associated with asthma development.
References:  4
Type:  Single nucleotide polymorphism
Species:  Human
Description:  The CXCR3-B splice variant is a 416 amino acid receptor with a longer N-terminal. It differs from CXCR3-A in its signalling properties by activating AC and increasing cAMP levels as well as being associated with reduced DNA synthesis and increased apoptosis. CXCR3-A and CXCR3-B are differentially expressed on subsets of endothelial cells and differentially recognise CXCL4 (platelet factor 4).
References:  15

References

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1. Aksoy MO, Yang Y, Ji R, Reddy PJ, Shahabuddin S, Litvin J, Rogers TJ, Kelsen SG. (2005) CXCR3 Surface Expression in Human Airway Epithelial Cells: Cell Cycle Dependence and Effect on Cell Proliferation. Am J Physiol Lung Cell Mol Physiol,: -. [PMID:16339779]

2. Brightling CE, Kaur D, Berger P, Morgan AJ, Wardlaw AJ, Bradding P. (2005) Differential expression of CCR3 and CXCR3 by human lung and bone marrow-derived mast cells: implications for tissue mast cell migration. J Leukoc Biol, 77 (5): 759-66. [PMID:15673545]

3. Cannon A, Thompson CM, Maurer HC, Atri P, Bhatia R, West S, Ghersi D, Olive KP, Kumar S, Batra SK. (2020) CXCR3 and Cognate Ligands are Associated with Immune Cell Alteration and Aggressiveness of Pancreatic Ductal Adenocarcinoma. Clin Cancer Res, 26 (22): 6051-6063. [PMID:32873571]

4. Cheong HS, Park CS, Kim LH, Park BL, Uh ST, Kim YH, Lym GI, Lee JY, Lee JK, Kim HT et al.. (2005) CXCR3 polymorphisms associated with risk of asthma. Biochem Biophys Res Commun, 334 (4): 1219-25. [PMID:16043121]

5. Christensen JE, Nansen A, Moos T, Lu B, Gerard C, Christensen JP, Thomsen AR. (2004) Efficient T-cell surveillance of the CNS requires expression of the CXC chemokine receptor 3. J Neurosci, 24 (20): 4849-58. [PMID:15152045]

6. Colvin RA, Campanella GS, Sun J, Luster AD. (2004) Intracellular domains of CXCR3 that mediate CXCL9, CXCL10, and CXCL11 function. J Biol Chem, 279 (29): 30219-27. [PMID:15150261]

7. Flynn G, Maru S, Loughlin J, Romero IA, Male D. (2003) Regulation of chemokine receptor expression in human microglia and astrocytes. J Neuroimmunol, 136 (1-2): 84-93. [PMID:12620646]

8. Heise CE, Pahuja A, Hudson SC, Mistry MS, Putnam AL, Gross MM, Gottlieb PA, Wade WS, Kiankarimi M, Schwarz D et al.. (2005) Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J Pharmacol Exp Ther, 313 (3): 1263-71. [PMID:15761110]

9. Huber TB, Reinhardt HC, Exner M, Burger JA, Kerjaschki D, Saleem MA, Pavenstädt H. (2002) Expression of functional CCR and CXCR chemokine receptors in podocytes. J Immunol, 168 (12): 6244-52. [PMID:12055238]

10. Jinquan T, Jing C, Jacobi HH, Reimert CM, Millner A, Quan S, Hansen JB, Dissing S, Malling HJ, Skov PS et al.. (2000) CXCR3 expression and activation of eosinophils: role of IFN-gamma-inducible protein-10 and monokine induced by IFN-gamma. J Immunol, 165 (3): 1548-56. [PMID:10903763]

11. Johnson M, Li AR, Liu J, Fu Z, Zhu L, Miao S, Wang X, Xu Q, Huang A, Marcus A et al.. (2007) Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett, 17 (12): 3339-43. [PMID:17448658]

12. Kelsen SG, Aksoy MO, Yang Y, Shahabuddin S, Litvin J, Safadi F, Rogers TJ. (2004) The chemokine receptor CXCR3 and its splice variant are expressed in human airway epithelial cells. Am J Physiol Lung Cell Mol Physiol, 287: L584-L591. [PMID:15155273]

13. Kivisäkk P, Trebst C, Lee JC, Tucky BH, Rudick RA, Campbell JJ, Ransohoff RM. (2003) Expression of CCR2, CCR5, and CXCR3 by CD4+ T cells is stable during a 2-year longitudinal study but varies widely between individuals. J Neurovirol, 9 (3): 291-9. [PMID:12775413]

14. Kouroumalis A, Nibbs RJ, Aptel H, Wright KL, Kolios G, Ward SG. (2005) The chemokines CXCL9, CXCL10, and CXCL11 differentially stimulate G alpha i-independent signaling and actin responses in human intestinal myofibroblasts. J Immunol, 175 (8): 5403-11. [PMID:16210647]

15. Lasagni L, Francalanci M, Annunziato F, Lazzeri E, Giannini S, Cosmi L, Sagrinati C, Mazzinghi B, Orlando C, Maggi E et al.. (2003) An alternatively spliced variant of CXCR3 mediates the inhibition of endothelial cell growth induced by IP-10, Mig, and I-TAC, and acts as functional receptor for platelet factor 4. J Exp Med, 197 (11): 1537-49. [PMID:12782716]

16. Lisignoli G, Toneguzzi S, Piacentini A, Cattini L, Lenti A, Tschon M, Cristino S, Grassi F, Facchini A. (2003) Human osteoblasts express functional CXC chemokine receptors 3 and 5: activation by their ligands, CXCL10 and CXCL13, significantly induces alkaline phosphatase and beta-N-acetylhexosaminidase release. J Cell Physiol, 194 (1): 71-9. [PMID:12447991]

17. Lisignoli G, Toneguzzi S, Piacentini A, Cristino S, Cattini L, Grassi F, Facchini A. (2004) Recruitment and proliferation of T lymphocytes is supported by IFNgamma- and TNFalpha-activated human osteoblasts: Involvement of CD54 (ICAM-1) and CD106 (VCAM-1) adhesion molecules and CXCR3 chemokine receptor. J Cell Physiol, 198 (3): 388-98. [PMID:14755544]

18. Loetscher M, Loetscher P, Brass N, Meese E, Moser B. (1998) Lymphocyte-specific chemokine receptor CXCR3: regulation, chemokine binding and gene localization. Eur J Immunol, 28 (11): 3696-705. [PMID:9842912]

19. Meyer EA, Äänismaa P, Ertel EA, Hühn E, Strasser DS, Rey M, Murphy MJ, Martinic MM, Pouzol L, Froidevaux S et al.. (2023) Discovery of Clinical Candidate ACT-777991, a Potent CXCR3 Antagonist for Antigen-Driven and Inflammatory Pathologies. J Med Chem, 66 (6): 4179-4196. [PMID:36883854]

20. Meyer EA, Äänismaa P, Froidevaux S, Keller M, Piali L, Caroff E. (2022) Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases. J Med Chem, 65 (17): 11513-11532. [PMID:35947786]

21. Nanki T, Lipsky PE. (2000) Lack of correlation between chemokine receptor and T(h)1/T(h)2 cytokine expression by individual memory T cells. Int Immunol, 12 (12): 1659-67. [PMID:11099305]

22. Ondeykal JG, Herath KB, Jayasuriya H, Polishook JD, Bills GF, Dombrowski AW, Mojena M, Koch G, DiSalvo J, DeMartino J et al.. (2005) Discovery of structurally diverse natural product antagonists of chemokine receptor CXCR3. Mol Divers, 9 (1-3): 123-9. [PMID:15789559]

23. Qin S, Rottman JB, Myers P, Kassam N, Weinblatt M, Loetscher M, Koch AE, Moser B, Mackay CR. (1998) The chemokine receptors CXCR3 and CCR5 mark subsets of T cells associated with certain inflammatory reactions. J Clin Invest, 101 (4): 746-54. [PMID:9466968]

24. Rappert A, Biber K, Nolte C, Lipp M, Schubel A, Lu B, Gerard NP, Gerard C, Boddeke HW, Kettenmann H. (2002) Secondary lymphoid tissue chemokine (CCL21) activates CXCR3 to trigger a Cl- current and chemotaxis in murine microglia. J Immunol, 168 (7): 3221-6. [PMID:11907075]

25. Sallusto F, Lenig D, Mackay CR, Lanzavecchia A. (1998) Flexible programs of chemokine receptor expression on human polarized T helper 1 and 2 lymphocytes. J Exp Med, 187 (6): 875-83. [PMID:9500790]

26. Soto H, Wang W, Strieter RM, Copeland NG, Gilbert DJ, Jenkins NA, Hedrick J, Zlotnik A. (1998) The CC chemokine 6Ckine binds the CXC chemokine receptor CXCR3. Proc Natl Acad Sci USA, 95 (14): 8205-10. [PMID:9653165]

27. Sørensen TL, Roed H, Sellebjerg F. (2002) Chemokine receptor expression on B cells and effect of interferon-beta in multiple sclerosis. J Neuroimmunol, 122 (1-2): 125-31. [PMID:11777551]

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