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CCR3

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 60

Nomenclature: CCR3

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 7 355 3p21.31 CCR3 C-C motif chemokine receptor 3 12,14,43
Mouse 7 359 9 75.05 cM Ccr3 C-C motif chemokine receptor 3 21
Rat 7 359 8q32 Ccr3 C-C motif chemokine receptor 3 26
Previous and Unofficial Names Click here for help
CC CKR3 [12,14] | MIP-1αRL-2 (mouse) [21] | CKR3 | CC-CKR-3 | CD193 | chemokine (C-C motif) receptor 3
Database Links Click here for help
Specialist databases
GPCRdb ccr3_human (Hs), ccr3_mouse (Mm), ccr3_rat (Rn)
Other databases
Alphafold P51677 (Hs), P51678 (Mm), O54814 (Rn)
ChEMBL Target CHEMBL3473 (Hs), CHEMBL3406 (Mm), CHEMBL3928 (Rn)
Ensembl Gene ENSG00000183625 (Hs), ENSMUSG00000035448 (Mm), ENSRNOG00000006736 (Rn)
Entrez Gene 1232 (Hs), 12771 (Mm), 117027 (Rn)
Human Protein Atlas ENSG00000183625 (Hs)
KEGG Gene hsa:1232 (Hs), mmu:12771 (Mm), rno:117027 (Rn)
OMIM 601268 (Hs)
Pharos P51677 (Hs)
RefSeq Nucleotide NM_001837 (Hs), NM_009914 (Mm), NM_053958 (Rn)
RefSeq Protein NP_001828 (Hs), NP_034044 (Mm), NP_446410 (Rn)
UniProtKB P51677 (Hs), P51678 (Mm), O54814 (Rn)
Wikipedia CCR3 (Hs)
Natural/Endogenous Ligands Click here for help
CCL15 {Sp: Human}
CCL5 {Sp: Human}
CCL7 {Sp: Human}
CCL11 {Sp: Human}
CCL13 {Sp: Human}
CCL8 {Sp: Human}
CCL24 {Sp: Human}
CCL26 {Sp: Human}
CCL2 {Sp: Human}
CCL28 {Sp: Human}
CCL11 {Sp: Mouse}
CCL7 {Sp: Mouse}
CCL8 {Sp: Mouse}
CCL24 {Sp: Mouse}
CCL2 {Sp: Mouse}
CCL28 {Sp: Mouse}
CCL5 {Sp: Mouse, Rat}
CCL7 {Sp: Rat}
CCL11 {Sp: Rat}
CCL2 {Sp: Rat}
CXCL9 {Sp: Human}
CXCL10 {Sp: Human}
CXCL11 {Sp: Human}
CXCL9 {Sp: Mouse}
CXCL10 {Sp: Mouse}
CXCL11 {Sp: Mouse}
CXCL10 {Sp: Rat}
Comments: CCL11, CCL24 and CCL26 are the principal endogenous agonists

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Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CCL11 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 9.7 – 10.0 pKi 14
⤷ pKi 9.7 – 10.0 [14]
CCL11 {Sp: Mouse} Peptide Immunopharmacology Ligand Hs Full agonist 9.5 – 10.0 pKi 14
⤷ pKi 9.5 – 10.0 [14]
CCL5 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.5 – 9.3 pKi 14
⤷ pKi 8.5 – 9.3 [14]
CCL7 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.6 – 9.2 pKi 14
⤷ pKi 8.6 – 9.2 [14]
CCL2 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.2 – 7.8 pKi 14
⤷ pKi 7.2 – 7.8 [14]
CCL13 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.7 – 10.3 pIC50 33,44
⤷ pIC50 8.7 – 10.3 [33,44]
CCL11 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.7 – 9.0 pIC50 15,29,33,41,44
⤷ pIC50 8.7 – 9.0 (IC50 1.99x10-9 – 1x10-9 M) [15,29,33,41,44]
CCL24 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.0 – 9.4 pIC50 33,38
⤷ pIC50 8.0 – 9.4 [33,38]
CCL15 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.6 pIC50 13
⤷ pIC50 8.6 [13]
CCL26 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.9 – 8.9 pIC50 29,33,38
⤷ pIC50 7.9 – 8.9 [29,33,38]
HIV-Tat Peptide Click here for species-specific activity table Hs Full agonist 7.2 pIC50 2
⤷ pIC50 7.2 [2]
CCL8 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist - -
⤷
CCL28 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist - -
⤷
Agonist Comments
It has been shown that CCL8 (MCP-2) is a ligand for the CCR3 receptor [23].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]CCL11 (human) Peptide Ligand is labelled Ligand is radioactive Hs Antagonist 8.3 pKd 46
⤷ pKd 8.3 (Kd 5.01x10-9 M) [46]
[3H]banyu (I) Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Inverse agonist 8.3 pKd 46
⤷ pKd 8.3 [46]
banyu (I) Small molecule or natural product Hs Inverse agonist 8.5 pKi 46
⤷ pKi 8.5 (Ki 3.16x10-9 M) [46]
lazucirnon Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 8.5 pKi 18
⤷ pKi 8.5 (Ki 3.2x10-9 M) [18]
Description: Dissociation constant determined in a scintillation proximity binding assay using recombinant human [125]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3.
AZD3778 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 pKi 6
⤷ pKi 8.2 (Ki 6.3x10-9 M) [6]
Description: Assay using sodium salt of the compound
BMS compound 87b Small molecule or natural product Hs Antagonist 8.1 pKi 45
⤷ pKi 8.1 (Ki 7.94x10-9 M) [45]
RO116-9132/238 Small molecule or natural product Hs Antagonist 9.0 pIC50 9
⤷ pIC50 9.0 [9]
RO320-2947/001 Small molecule or natural product Hs Antagonist 8.4 pIC50 9
⤷ pIC50 8.4 [9]
RO330-0802/001 Small molecule or natural product Hs Antagonist 8.3 pIC50 9
⤷ pIC50 8.3 [9]
Met-Ckβ7 Peptide Hs Antagonist 8.2 pIC50 36
⤷ pIC50 8.2 [36]
GW766994 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 8.0 pIC50 39
⤷ pIC50 8.0 (IC50 1x10-8 M) [39]
YM-355179 Small molecule or natural product Hs Antagonist 7.6 – 8.1 pIC50 33
⤷ pIC50 7.6 – 8.1 [33]
CCL18 {Sp: Human} Peptide Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.5 – 8.5 pIC50 30
⤷ pIC50 6.5 – 8.5 (IC50 3.176x10-7 – 2.9x10-9 M) [30]
RO116-4875/608 Small molecule or natural product Hs Antagonist 7.2 pIC50 9
⤷ pIC50 7.2 [9]
UCB35625 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 pIC50 41
⤷ pIC50 7.0 (IC50 9.36x10-8 M) [41]
Description: Measuring antagonism of CCL11-induced chemotaxis in vitro.
CXCL10 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Antagonist - -
⤷
CXCL11 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Antagonist - -
⤷
CXCL9 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Antagonist - -
⤷
Antagonist Comments
CCL9 and CCL10 are CCR3 antagonists.
Immunopharmacology Comments
CCR3 is one of more than 20 distinct chemokine receptors expressed in human leukocytes. Chemokines primarily act to promote leukocyte chemotaxis to sites of inflammation.
Cell Type Associations
Immuno Cell Type:  T cells
Cell Ontology Term:   T-helper 2 cell (CL:0000546)
Comment:  CCR3 is expressed on mast cells, basophils, and Th2 lymphocytes.
References:  35
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   basophil (CL:0000767)
eosinophil (CL:0000771)
Comment:  CCR3 is highly expressed on eosinophils, and is the promary receptor mediating their differentiation, chemotaxis and degranulation. It is also expressed on basophils, mast cells, and Th2 lymphocytes.
References:  1,31,35
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  CCR3 is expressed on mast cells, basophils, and Th2 lymphocytes
References:  35
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cytokine production & signalling
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Calcium channel
References: 
Tissue Distribution Click here for help
Platelets.
Species:  Human
Technique:  RT-PCR and flow cytometry.
References:  11
Basophils.
Species:  Human
Technique:  RT-PCR.
References:  25
Blood dendritic cells.
Species:  Human
Technique:  RT-PCR.
References:  4
Microvascular endothelial cells.
Species:  Human
Technique:  RNase protection assay.
References:  42
Microglia.
Species:  Human
Technique:  Flow cytometry.
References:  3
Primary adult microglia and astrocytes.
Species:  Human
Technique:  Flow cytometry.
References:  16
Th2-type lymphocytes.
Species:  Human
Technique:  Flow cytometry.
References:  22
Th2-type lymphocytes.
Species:  Human
Technique:  RT-PCR.
References:  34
Basophils and eosinophils.
Species:  Human
Technique:  Flow cytometry and Northern blotting.
References:  44
Basophils.
Species:  Human
Technique:  Flow cytometry.
References:  25,37
Osteoblasts.
Species:  Rat
Technique:  RT-PCR.
References:  47
Spleen.
Species:  Rat
Technique:  Northern blotting.
References:  26
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 Ca2+ levels in human CD34+ blood progenitor cells endogenously expressing the CCR3 receptor.
Species:  Human
Tissue:  CD34+ blood progenitor cells.
Response measured:  Ca2+ mobilisation.
References:  31
Measurement of chemotaxis of CD34+ blood progenitor cells endogenously expressing the CCR3 receptor.
Species:  Human
Tissue:  CD34+ blood progenitor cells.
Response measured:  Chemotaxis.
References:  31
Detection of HIV-1 fusion in HeLa cells transfected with CD4 and the CCR3 receptor.
Species:  Human
Tissue:  HeLa-CD4 cells.
Response measured:  HIV-1 fusion and infection.
References:  10
Measurement of chemotaxis of eosinophils endogenously expressing the CCR3 receptor.
Species:  Human
Tissue:  Eosinophils.
Response measured:  Chemotaxis.
References:  17,29,36
Measurement of MAP kinase activity in eosinophils endogenously expressing the CCR3 receptor.
Species:  Human
Tissue:  Eosinophils.
Response measured:  Activation of MAP kinases.
References:  7,27
Measurement of Ca2+ levels in eosinophils endogenously expressing the CCR3 receptor.
Species:  Human
Tissue:  Eosinophils.
Response measured:  Ca2+ influx.
References:  19,36
Measurement of superoxide anion levels in eosinophils endogenously expressing the CCR3 receptor.
Species:  Human
Tissue:  Eosinophils.
Response measured:  Superoxide anion production.
References:  5
Physiological Functions Click here for help
Chemotaxis.
Species:  Human
Tissue:  Leukocytes.
References:  17
Degranulation.
Species:  Human
Tissue:  Eosinophils.
References:  5,19
Angiogenesis.
Species:  Rat
Tissue:  Aortic rings.
References:  42
Eosinophil recruitment.
Species:  Mouse
Tissue:  In vivo.
References:  8,24,32,40
Physiological Consequences of Altering Gene Expression Click here for help
CCR3 knockout mice with induced skin inflammation exhibit impaired recruitment of eosinophils to lung parenchyma and bronchoalveolar lavage. Cholinergic stimulation did not result in airway hyperresponsiveness.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  32
CCR3 receptor knockout mice with induced pulmonary inflammation exhibit reduced trafficking of eosinophils from the blood into the lung parenchyma and increased numbers of intraepithelial mast cells in the trachea. Cholinergic stimulation resulted in airway hyperresponsiveness.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  24
CCR3 receptor knockout mice have decreased levels of eosinophils in the blood, spleen and jejunum. Following induced inflammation, the knockout mice exhibit a 6-fold increase in the number of eosinophils in the blood compared to the wild-type.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  40
CCR3 receptor knockout mice lack allergen-induced eosinophil accumulation in the esophagus normally seen with the wild-type eosinophilic esophagitis mouse model.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  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
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0002334 abnormal airway responsiveness PMID: 11877470 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0002602 abnormal eosinophil cell number PMID: 11830666 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0002465 abnormal eosinophil physiology PMID: 11830666  11877470 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0002423 abnormal mast cell physiology PMID: 11830666 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0005012 decreased eosinophil cell number PMID: 11830666  11877470 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0008724 impaired eosinophil migration PMID: 11830666 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0008723 impaired eosinophil recruitment PMID: 11830666  11877470 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0001952 increased airway responsiveness PMID: 11830666 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0005011 increased eosinophil cell number PMID: 11830666 
Ccr3tm1Cge Ccr3tm1Cge/Ccr3tm1Cge
involves: 129S4/SvJae * BALB/c		 MGI:104616  MP:0008764 increased mast cell degranulation PMID: 11830666 
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  A Thr51 -> Cys polymorphism has been identified in humans and may be associated with the development of asthma.
Amino acid change:  T51C
References:  20
Type:  Single nucleotide polymorphism
Species:  Human
Description:  A Cys218 -> Ser polymorphism in the CCR3 gene has been identified in human, perhaps with reduced function at the protein level.
Amino acid change:  C218S
References:  28

References

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1. Ahmadi Z, Hassanshahi G, Khorramdelazad H, Zainodini N, Koochakzadeh L. (2016) An Overlook to the Characteristics and Roles Played by Eotaxin Network in the Pathophysiology of Food Allergies: Allergic Asthma and Atopic Dermatitis. Inflammation, 39 (3): 1253-67. [PMID:26861136]

2. Albini A, Ferrini S, Benelli R, Sforzini S, Giunciuglio D, Aluigi MG, Proudfoot AE, Alouani S, Wells TN, Mariani G et al.. (1998) HIV-1 Tat protein mimicry of chemokines. Proc Natl Acad Sci USA, 95 (22): 13153-8. [PMID:9789057]

3. Albright AV, Shieh JT, Itoh T, Lee B, Pleasure D, O'Connor MJ, Doms RW, González-Scarano F. (1999) Microglia express CCR5, CXCR4, and CCR3, but of these, CCR5 is the principal coreceptor for human immunodeficiency virus type 1 dementia isolates. J Virol, 73 (1): 205-13. [PMID:9847323]

4. Ayehunie S, Garcia-Zepeda EA, Hoxie JA, Horuk R, Kupper TS, Luster AD, Ruprecht RM. (1997) Human immunodeficiency virus-1 entry into purified blood dendritic cells through CC and CXC chemokine coreceptors. Blood, 90 (4): 1379-86. [PMID:9269754]

5. Badewa AP, Hudson CE, Heiman AS. (2002) Regulatory effects of eotaxin, eotaxin-2, and eotaxin-3 on eosinophil degranulation and superoxide anion generation. Exp Biol Med (Maywood), 227 (8): 645-51. [PMID:12192108]

6. Bahl A, Barton P, Bowers K, Brough S, Evans R, Luckhurst CA, Mochel T, Perry MW, Rigby A, Riley RJ et al.. (2012) The discovery of CCR3/H1 dual antagonists with reduced hERG risk. Bioorg Med Chem Lett, 22 (21): 6688-93. [PMID:23031591]

7. Bandeira-Melo C, Phoofolo M, Weller PF. (2001) Extranuclear lipid bodies, elicited by CCR3-mediated signaling pathways, are the sites of chemokine-enhanced leukotriene C4 production in eosinophils and basophils. J Biol Chem, 276 (25): 22779-87. [PMID:11274187]

8. Blanchard C, Wang N, Stringer KF, Mishra A, Fulkerson PC, Abonia JP, Jameson SC, Kirby C, Konikoff MR, Collins MH et al.. (2006) Eotaxin-3 and a uniquely conserved gene-expression profile in eosinophilic esophagitis. J Clin Invest, 116 (2): 536-47. [PMID:16453027]

9. Bryan SA, Jose PJ, Topping JR, Wilhelm R, Soderberg C, Kertesz D, Barnes PJ, Williams TJ, Hansel TT, Sabroe I. (2002) Responses of leukocytes to chemokines in whole blood and their antagonism by novel CC-chemokine receptor 3 antagonists. Am J Respir Crit Care Med, 165 (12): 1602-9. [PMID:12070060]

10. Choe H, Farzan M, Sun Y, Sullivan N, Rollins B, Ponath PD, Wu L, Mackay CR, LaRosa G, Newman W et al.. (1996) The beta-chemokine receptors CCR3 and CCR5 facilitate infection by primary HIV-1 isolates. Cell, 85 (7): 1135-48. [PMID:8674119]

11. Clemetson KJ, Clemetson JM, Proudfoot AE, Power CA, Baggiolini M, Wells TN. (2000) Functional expression of CCR1, CCR3, CCR4, and CXCR4 chemokine receptors on human platelets. Blood, 96 (13): 4046-54. [PMID:11110672]

12. Combadiere C, Ahuja SK, Murphy PM. (1995) Cloning and functional expression of a human eosinophil CC chemokine receptor. J Biol Chem, 270 (28): 16491-4. [PMID:7622448]

13. Coulin F, Power CA, Alouani S, Peitsch MC, Schroeder JM, Moshizuki M, Clark-Lewis I, Wells TN. (1997) Characterisation of macrophage inflammatory protein-5/human CC cytokine-2, a member of the macrophage-inflammatory-protein family of chemokines. Eur J Biochem, 248 (2): 507-15. [PMID:9346309]

14. Daugherty BL, Siciliano SJ, DeMartino JA, Malkowitz L, Sirotina A, Springer MS. (1996) Cloning, expression, and characterization of the human eosinophil eotaxin receptor. J Exp Med, 183 (5): 2349-54. [PMID:8642344]

15. Duggal P, An P, Beaty TH, Strathdee SA, Farzadegan H, Markham RB, Johnson L, O'Brien SJ, Vlahov D, Winkler CA. (2003) Genetic influence of CXCR6 chemokine receptor alleles on PCP-mediated AIDS progression among African Americans. Genes Immun, 4 (4): 245-50. [PMID:12761559]

16. 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]

17. Forssmann U, Uguccioni M, Loetscher P, Dahinden CA, Langen H, Thelen M, Baggiolini M. (1997) Eotaxin-2, a novel CC chemokine that is selective for the chemokine receptor CCR3, and acts like eotaxin on human eosinophil and basophil leukocytes. J Exp Med, 185 (12): 2171-6. [PMID:9182688]

18. Frank M, Haerberle H, Henry M, Pachur T, Santagostino M, Stertz U, Trebling T, Werthmann U. (2012) Co-crystals and salts of ccr3-inhibitors. Patent number: WO2012045803A1. Assignee: Boehringer Ingelheim International Gmbh. Priority date: 07/10/2010. Publication date: 12/04/2012.

19. Fujisawa T, Kato Y, Nagase H, Atsuta J, Terada A, Iguchi K, Kamiya H, Morita Y, Kitaura M, Kawasaki H et al.. (2000) Chemokines induce eosinophil degranulation through CCR-3. J Allergy Clin Immunol, 106 (3): 507-13. [PMID:10984371]

20. Fukunaga K, Asano K, Mao XQ, Gao PS, Roberts MH, Oguma T, Shiomi T, Kanazawa M, Adra CN, Shirakawa T et al.. (2001) Genetic polymorphisms of CC chemokine receptor 3 in Japanese and British asthmatics. Eur Respir J, 17 (1): 59-63. [PMID:11307756]

21. Gao JL, Murphy PM. (1995) Cloning and differential tissue-specific expression of three mouse beta chemokine receptor-like genes, including the gene for a functional macrophage inflammatory protein-1 alpha receptor. J Biol Chem, 270: 17494-17501. [PMID:7542241]

22. Gerber BO, Zanni MP, Uguccioni M, Loetscher M, Mackay CR, Pichler WJ, Yawalkar N, Baggiolini M, Moser B. (1997) Functional expression of the eotaxin receptor CCR3 in T lymphocytes co-localizing with eosinophils. Curr Biol, 7 (11): 836-43. [PMID:9480044]

23. Heinemann A, Hartnell A, Stubbs VE, Murakami K, Soler D, LaRosa G, Askenase PW, Williams TJ, Sabroe I. (2000) Basophil responses to chemokines are regulated by both sequential and cooperative receptor signaling. J Immunol, 165 (12): 7224-33. [PMID:11120855]

24. Humbles AA, Lu B, Friend DS, Okinaga S, Lora J, Al-Garawi A, Martin TR, Gerard NP, Gerard C. (2002) The murine CCR3 receptor regulates both the role of eosinophils and mast cells in allergen-induced airway inflammation and hyperresponsiveness. Proc Natl Acad Sci USA, 99 (3): 1479-84. [PMID:11830666]

25. Iikura M, Miyamasu M, Yamaguchi M, Kawasaki H, Matsushima K, Kitaura M, Morita Y, Yoshie O, Yamamoto K, Hirai K. (2001) Chemokine receptors in human basophils: inducible expression of functional CXCR4. J Leukoc Biol, 70: 113-120. [PMID:11435493]

26. Jiang Y, Salafranca MN, Adhikari S, Xia Y, Feng L, Sonntag MK, deFiebre CM, Pennell NA, Streit WJ, Harrison JK. (1998) Chemokine receptor expression in cultured glia and rat experimental allergic encephalomyelitis. J Neuroimmunol, 86 (1): 1-12. [PMID:9655467]

27. Kampen GT, Stafford S, Adachi T, Jinquan T, Quan S, Grant JA, Skov PS, Poulsen LK, Alam R. (2000) Eotaxin induces degranulation and chemotaxis of eosinophils through the activation of ERK2 and p38 mitogen-activated protein kinases. Blood, 95 (6): 1911-7. [PMID:10706854]

28. Kato H, Tsuchiya N, Izumi S, Miyamasu M, Nakajima T, Kawasaki H, Hirai K, Tokunaga K. (1999) New variations of human CC-chemokine receptors CCR3 and CCR4. Genes Immun, 1 (2): 97-104. [PMID:11196669]

29. Kitaura M, Suzuki N, Imai T, Takagi S, Suzuki R, Nakajima T, Hirai K, Nomiyama H, Yoshie O. (1999) Molecular cloning of a novel human CC chemokine (Eotaxin-3) that is a functional ligand of CC chemokine receptor 3. J Biol Chem, 274 (39): 27975-80. [PMID:10488147]

30. Krohn SC, Bonvin P, Proudfoot AE. (2013) CCL18 exhibits a regulatory role through inhibition of receptor and glycosaminoglycan binding. PLoS ONE, 8 (8): e72321. [PMID:23951310]

31. Lamkhioued B, Abdelilah SG, Hamid Q, Mansour N, Delespesse G, Renzi PM. (2003) The CCR3 receptor is involved in eosinophil differentiation and is up-regulated by Th2 cytokines in CD34+ progenitor cells. J Immunol, 170 (1): 537-47. [PMID:12496441]

32. Ma W, Bryce PJ, Humbles AA, Laouini D, Yalcindag A, Alenius H, Friend DS, Oettgen HC, Gerard C, Geha RS. (2002) CCR3 is essential for skin eosinophilia and airway hyperresponsiveness in a murine model of allergic skin inflammation. J Clin Invest, 109 (5): 621-8. [PMID:11877470]

33. Morokata T, Suzuki K, Masunaga Y, Taguchi K, Morihira K, Sato I, Fujii M, Takizawa S, Torii Y, Yamamoto N et al.. (2006) A novel, selective, and orally available antagonist for CC chemokine receptor 3. J Pharmacol Exp Ther, 317 (1): 244-50. [PMID:16339911]

34. 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]

35. Neighbour H, Boulet LP, Lemiere C, Sehmi R, Leigh R, Sousa AR, Martin J, Dallow N, Gilbert J, Allen A et al.. (2014) Safety and efficacy of an oral CCR3 antagonist in patients with asthma and eosinophilic bronchitis: a randomized, placebo-controlled clinical trial. Clin Exp Allergy, 44 (4): 508-16. [PMID:24286456]

36. Nibbs RJ, Salcedo TW, Campbell JD, Yao XT, Li Y, Nardelli B, Olsen HS, Morris TS, Proudfoot AE, Patel VP et al.. (2000) C-C chemokine receptor 3 antagonism by the beta-chemokine macrophage inflammatory protein 4, a property strongly enhanced by an amino-terminal alanine-methionine swap. J Immunol, 164 (3): 1488-97. [PMID:10640766]

37. Ochensberger B, Tassera L, Bifrare D, Rihs S, Dahinden CA. (1999) Regulation of cytokine expression and leukotriene formation in human basophils by growth factors, chemokines and chemotactic agonists. Eur J Immunol, 29 (1): 11-22. [PMID:9933081]

38. Parody TR, Stone MJ. (2004) High level expression, activation, and antagonism of CC chemokine receptors CCR2 and CCR3 in Chinese hamster ovary cells. Cytokine, 27 (1): 38-46. [PMID:15207250]

39. Pease J, Horuk R. (2012) Chemokine receptor antagonists. J Med Chem, 55 (22): 9363-92. [PMID:22931505]

40. Pope SM, Zimmermann N, Stringer KF, Karow ML, Rothenberg ME. (2005) The eotaxin chemokines and CCR3 are fundamental regulators of allergen-induced pulmonary eosinophilia. J Immunol, 175 (8): 5341-50. [PMID:16210640]

41. Sabroe I, Peck MJ, Van Keulen BJ, Jorritsma A, Simmons G, Clapham PR, Williams TJ, Pease JE. (2000) A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry. J Biol Chem, 275 (34): 25985-92. [PMID:10854442]

42. Salcedo R, Young HA, Ponce ML, Ward JM, Kleinman HK, Murphy WJ, Oppenheim JJ. (2001) Eotaxin (CCL11) induces in vivo angiogenic responses by human CCR3+ endothelial cells. J Immunol, 166 (12): 7571-8. [PMID:11390513]

43. Samson M, Soularue P, Vassart G, Parmentier M. (1996) The genes encoding the human CC-chemokine receptors CC-CKR1 to CC-CKR5 (CMKBR1-CMKBR5) are clustered in the p21.3-p24 region of chromosome 3. Genomics, 36: 522-526. [PMID:8884276]

44. Uguccioni M, Mackay CR, Ochensberger B, Loetscher P, Rhis S, LaRosa GJ, Rao P, Ponath PD, Baggiolini M, Dahinden CA. (1997) High expression of the chemokine receptor CCR3 in human blood basophils. Role in activation by eotaxin, MCP-4, and other chemokines. J Clin Invest, 100 (5): 1137-43. [PMID:9276730]

45. Wacker DA, Santella 3rd JB, Gardner DS, Varnes JG, Estrella M, DeLucca GV, Ko SS, Tanabe K, Watson PS, Welch PK et al.. (2002) CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships. Bioorg Med Chem Lett, 12 (13): 1785-9. [PMID:12067561]

46. Wan Y, Jakway JP, Qiu H, Shah H, Garlisi CG, Tian F, Ting P, Hesk D, Egan RW, Billah MM et al.. (2002) Identification of full, partial and inverse CC chemokine receptor 3 agonists using [35S]GTPgammaS binding. Eur J Pharmacol, 456 (1-3): 1-10. [PMID:12450563]

47. Yano S, Mentaverri R, Kanuparthi D, Bandyopadhyay S, Rivera A, Brown EM, Chattopadhyay N. (2005) Functional expression of beta-chemokine receptors in osteoblasts: role of regulated upon activation, normal T cell expressed and secreted (RANTES) in osteoblasts and regulation of its secretion by osteoblasts and osteoclasts. Endocrinology, 146 (5): 2324-35. [PMID:15718270]

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