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CCR1

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 58

Nomenclature: CCR1

Family: Chemokine receptors

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 CCR1 C-C motif chemokine receptor 1 30,33
Mouse 7 355 9 75.05 cM Ccr1 C-C motif chemokine receptor 1 8
Rat 7 355 8q32 Ccr1 C-C motif chemokine receptor 1
Previous and Unofficial Names Click here for help
CC CKR1 | CKR1 | MIP-1α/RANTES | MIP-1αR | CD191 | CMKBR1 | MIP1aR | macrophage inflammatory protein-1 alpha receptor
Database Links Click here for help
Specialist databases
GPCRdb ccr1_human (Hs), ccr1_mouse (Mm), q9jly8_rat (Rn)
Other databases
Alphafold
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
CCL14 {Sp: Human}
CCL15 {Sp: Human}
CCL23 {Sp: Human}
CCL3 {Sp: Human}
CCL5 {Sp: Human}
CCL7 {Sp: Human}
CCL13 {Sp: Human}
CCL8 {Sp: Human}
CCL16 {Sp: Human}
CCL4 {Sp: Human}
CCL3 {Sp: Mouse}
CCL7 {Sp: Mouse}
CCL8 {Sp: Mouse}
CCL4 {Sp: Mouse}
CCL5 {Sp: Mouse, Rat}
CCL3 {Sp: Rat}
CCL7 {Sp: Rat}
CCL4 {Sp: Rat}
Comments: CCL15 and CCL23 are the principal endogenous agonists

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]CCL2 (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 9.4 pKd 32
pKd 9.4 [32]
[125I]CCL7 (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 9.2 pKd 2
pKd 9.2 (Kd 7x10-10 M) [2]
[125I]CCL3 (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.0 – 8.8 pKd 2,12,32
pKd 8.0 – 8.8 (Kd 1x10-8 – 1.58x10-9 M) [2,12,32]
[125I]CCL8 (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.3 pKd 12
pKd 8.3 [12]
[125I]CCL5 (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.2 pKd 32
pKd 8.2 (Kd 7x10-9 M) [32]
CCL3 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.8 – 10.2 pKi 3,5,15,38
pKi 7.8 – 10.2 [3,5,15,38]
CCL23 {Sp: Human} Peptide Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.9 pKi 3
pKi 8.9 [3]
BP-CCL3 Peptide Click here for species-specific activity table Hs Full agonist 8.8 pKi 38
pKi 8.8 [38]
CCL7 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 8.1 pKi 3,13
pKi 8.1 [3,13]
CCL5 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 6.8 – 8.2 pKi 5,15
pKi 6.8 – 8.2 [5,15]
CCL14 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.4 pKi 3
pKi 7.4 [3]
Flu-CCL3 Peptide Click here for species-specific activity table Ligand is labelled Hs Full agonist 7.1 pKi 38
pKi 7.1 [38]
CCL15 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Full agonist 7.9 pIC50 7
pIC50 7.9 [7]
CCL13 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Agonist - -
CCL8 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Agonist - -
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CP-481,715 Small molecule or natural product Hs Antagonist 8.0 pKd 11
pKd 8.0 (Kd 9.2x10-9 M) [11]
BX 471 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 8.2 – 9.0 pKi 24
pKi 8.2 – 9.0 (Ki 6.31x10-9 – 1x10-9 M) [24]
CCL4 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Antagonist 7.1 – 7.8 pKi 3,5
pKi 7.1 – 7.8 [3,5]
MLN-3897 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.1 pIC50
pIC50 9.1 (IC50 8x10-10 M)
BMS-817399 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 9.0 pIC50 31
pIC50 9.0 (IC50 1x10-9 M) [31]
Description: Displacement of [125I]MIP-1α from CCR1 in human THP-1 cells.
compound 2b-1 [PMID: 12614873] Small molecule or natural product Hs Antagonist 8.7 pIC50 27
pIC50 8.7 [27]
vMIP-II Peptide Click here for species-specific activity table Hs Antagonist 8.1 pIC50 20
pIC50 8.1 [20]
UCB35625 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 pIC50 28
pIC50 8.0 (IC50 9.6x10-9 M) [28]
Description: Measuring antagonism of CCL3-induced chemotaxis in vitro.
CCL18 {Sp: Human} Peptide Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.1 – 6.1 pIC50 22
pIC50 6.1 – 6.1 (IC50 8.25x10-7 – 8.03x10-7 M) [22]
CCX354 Small molecule or natural product Immunopharmacology Ligand Hs Antagonist - - 23
[23]
Immunopharmacology Comments
CCR1 is one of more than 20 distinct chemokine receptors expressed in human leukocytes. Chemokines primarily act to promote leukocyte chemotaxis to sites of inflammation.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Calcium channel
References:  19
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Phospholipase C stimulation
Comments:  PLC activation mediates cell chemotaxis [21].
References:  21
Tissue Distribution Click here for help
Basophils and eosinophils.
Species:  Human
Technique:  Flow cytometry.
References:  35
Platelets.
Species:  Human
Technique:  RT-PCR and flow cytomery.
References:  4
Tonsil B lymphocytes.
Species:  Human
Technique:  RT-PCR.
References:  6
Blood derived mast cells.
Species:  Human
Technique:  RNase protection assay.
References:  18
Basophils.
Species:  Human
Technique:  RT-PCR and flow cytometry.
References:  17
Blood dendritic cells.
Species:  Human
Technique:  RT-PCR.
References:  1
Microvascular endothelial cells.
Species:  Human
Technique:  RNase protection assay.
References:  29
Bone marrow stromal cells (BMSCs).
Species:  Human
Technique:  Flow cytometry and RT-PCR.
References:  16
Macrophages.
Species:  Human
Technique:  Western blotting, fluorescence activated cell sorting analysis, RT-PCR and in situ hybridisation.
References:  36
Vascular smooth muscle cells.
Species:  Human
Technique:  RT-PCR.
References:  14
T cells.
Species:  Mouse
Technique:  Microarray analysis, RNase protection assay, Western blotting, and in vitro chemokine transmigration assays.
References:  26
Hippocampal neurons.
Species:  Rat
Technique:  RT-PCR.
References:  25
Osteoblasts.
Species:  Rat
Technique:  RT-PCR.
References:  37
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 K562 cells transfected with the mouse CCR1 receptor.
Species:  Mouse
Tissue:  K562 cells.
Response measured:  Ca2+ mobilisation.
References:  8
Measurement of chemotaxis of blood-derived mast cells endogenously expressing the CCR1 receptor.
Species:  Human
Tissue:  Mast cells.
Response measured:  Chemotaxis.
References:  18
Measurement of Ca2+ levels in human vascular smooth muscle cells (VSMCs) endogenously expressing the CCR2 receptor.
Species:  Human
Tissue:  VSMCs.
Response measured:  Increase in Ca2+ concentration.
References:  14
Measurement of PLC activity and chemotaxis of HOS cells endogenously expressing the CCR1 receptor.
Species:  Human
Tissue:  HOS cells.
Response measured:  PTX-sensitive PLC activation and chemotaxis.
References:  21
Measurement of Ca2+ levels in retanoic acid pre-treated human promyelocytic leukemia cell line, HL-60(Rx), endogenously expressing the CCR1 receptor.
Species:  Human
Tissue:  HL-60(Rx) cells.
Response measured:  Ca2+ mobilisation.
References:  3
Measurement of chemotaxis of retanoic acid pre-treated human promyelocytic leukemia cell line, HL-60(Rx), endogenously expressing the CCR1 receptor.
Species:  Human
Tissue:  HL-60(Rx) cells.
Response measured:  Chemotaxis.
References:  3
Physiological Functions Click here for help
Chemotaxis.
Species:  Human
Tissue:  Mast cells.
References:  18
Recruitment of T cells and macrophages.
Species:  Mouse
Tissue:  Kidney.
References:  34
Physiological Consequences of Altering Gene Expression Click here for help
CCR1 receptor knockout mice exhibit disordered trafficking and proliferation of myeloid progenitor cells as well as failed neutrophil chemotaxis in peripheral blood. In addition, CCR1 receptor-null mice show accelerated mortality when infected with a fungus known to be controlled by neutrophils.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  9
CCR1 receptor knockout mice exhibit prolonged rejection of cardiac allografts compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  10
CCR1 receptor knockout mice with nephrotoxic nephritis exhibit increased renal recruitment of CD4+ and CD8+ T cells and macrophages compared to wild-type mice with the disease. They also develop more severe glomerulonephritis, greater proteinuria and blood urea nitrogen, higher frequency of crescent formation, enhanced Th1 immune responses, delayed-type hypersensitivity responses and enhanced IFN-γ and TNF-α production.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  34
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
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
B6.129S4-Ccr1
MGI:104618  MP:0009858 abnormal cellular extravasation PMID: 16275892 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
B6.129S4-Ccr1
MGI:104618  MP:0003628 abnormal leukocyte adhesion PMID: 16275892 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
involves: 129S4/SvJae * C57BL/6
MGI:104618  MP:0002463 abnormal neutrophil physiology PMID: 9166425 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
B6.129S4-Ccr1
MGI:104618  MP:0000343 altered response to myocardial infarction PMID: 16275892 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
involves: C57BL/6
MGI:104618  MP:0000336 decreased mast cell number PMID: 15517609 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
involves: C57BL/6
MGI:104618  MP:0005614 decreased susceptibility to type III hypersensitivity reaction PMID: 15517609 
Ccr1tm1Cge Ccr1tm1Cge/Ccr1tm1Cge
involves: 129S4/SvJae
MGI:104618  MP:0008561 decreased tumor necrosis factor secretion PMID: 9329966 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
involves: 129S4/SvJae * C57BL/6
MGI:104618  MP:0002500 granulomatous inflammation PMID: 9166425 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
involves: 129S4/SvJae * C57BL/6
MGI:104618  MP:0001606 impaired hematopoiesis PMID: 9166425 
Ccr1tm1Cge Ccr1tm1Cge/Ccr1tm1Cge
involves: 129S4/SvJae
MGI:104618  MP:0008719 impaired neutrophil recruitment PMID: 9329966 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
involves: 129S4/SvJae * C57BL/6
MGI:104618  MP:0005399 increased susceptibility to fungal infection PMID: 9166425 
Ccr1tm1Gao Ccr1tm1Gao/Ccr1tm1Gao
involves: 129S4/SvJae * C57BL/6
MGI:104618  MP:0005027 increased susceptibility to parasitic infection PMID: 9166425 
Ccr1tm1Cge Ccr1tm1Cge/Ccr1tm1Cge
involves: 129S4/SvJae
MGI:104618  MP:0001861 lung inflammation PMID: 9329966 

References

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1. 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]

2. Ben-Baruch A, Xu L, Young PR, Bengali K, Oppenheim JJ, Wang JM. (1995) Monocyte chemotactic protein-3 (MCP3) interacts with multiple leukocyte receptors. C-C CKR1, a receptor for macrophage inflammatory protein-1 alpha/Rantes, is also a functional receptor for MCP3. J Biol Chem, 270 (38): 22123-8. [PMID:7545673]

3. Chou CC, Fine JS, Pugliese-Sivo C, Gonsiorek W, Davies L, Deno G, Petro M, Schwarz M, Zavodny PJ, Hipkin RW. (2002) Pharmacological characterization of the chemokine receptor, hCCR1 in a stable transfectant and differentiated HL-60 cells: antagonism of hCCR1 activation by MIP-1beta. Br J Pharmacol, 137 (5): 663-75. [PMID:12381680]

4. 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]

5. Combadiere C, Ahuja SK, Van Damme J, Tiffany HL, Gao JL, Murphy PM. (1995) Monocyte chemoattractant protein-3 is a functional ligand for CC chemokine receptors 1 and 2B. J Biol Chem, 270: 29671-29675. [PMID:8530354]

6. Corcione A, Tortolina G, Bonecchi R, Battilana N, Taborelli G, Malavasi F, Sozzani S, Ottonello L, Dallegri F, Pistoia V. (2002) Chemotaxis of human tonsil B lymphocytes to CC chemokine receptor (CCR) 1, CCR2 and CCR4 ligands is restricted to non-germinal center cells. Int Immunol, 14: 883-892. [PMID:12147625]

7. 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]

8. 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]

9. Gao JL, Wynn TA, Chang Y, Lee EJ, Broxmeyer HE, Cooper S, Tiffany HL, Westphal H, Kwon-Chung J, Murphy PM. (1997) Impaired host defense, hematopoiesis, granulomatous inflammation and type 1-type 2 cytokine balance in mice lacking CC chemokine receptor 1. J Exp Med, 185 (11): 1959-68. [PMID:9166425]

10. Gao W, Topham PS, King JA, Smiley ST, Csizmadia V, Lu B, Gerard CJ, Hancock WW. (2000) Targeting of the chemokine receptor CCR1 suppresses development of acute and chronic cardiac allograft rejection. J Clin Invest, 105 (1): 35-44. [PMID:10619859]

11. Gladue RP, Tylaska LA, Brissette WH, Lira PD, Kath JC, Poss CS, Brown MF, Paradis TJ, Conklyn MJ, Ogborne KT et al.. (2003) CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. J Biol Chem, 278 (42): 40473-80. [PMID:12909630]

12. Gong X, Gong W, Kuhns DB, Ben-Baruch A, Howard OM, Wang JM. (1997) Monocyte chemotactic protein-2 (MCP-2) uses CCR1 and CCR2B as its functional receptors. J Biol Chem, 272 (18): 11682-5. [PMID:9115216]

13. Habasque C, Aubry F, Jégou B, Samson M. (2002) Study of the HIV-1 receptors CD4, CXCR4, CCR5 and CCR3 in the human and rat testis. Mol Hum Reprod, 8 (5): 419-25. [PMID:11994538]

14. Hayes IM, Jordan NJ, Towers S, Smith G, Paterson JR, Earnshaw JJ, Roach AG, Westwick J, Williams RJ. (1998) Human vascular smooth muscle cells express receptors for CC chemokines. Arterioscler Thromb Vasc Biol, 18 (3): 397-403. [PMID:9514408]

15. Hesselgesser J, Ng HP, Liang M, Zheng W, May K, Bauman JG, Monahan S, Islam I, Wei GP, Ghannam A et al.. (1998) Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor. J Biol Chem, 273 (25): 15687-92. [PMID:9624164]

16. Honczarenko M, Le Y, Swierkowski M, Ghiran I, Glodek AM, Silberstein LE. (2006) Human bone marrow stromal cells express a distinct set of biologically functional chemokine receptors. Stem Cells, 24 (4): 1030-41. [PMID:16253981]

17. 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]

18. Juremalm M, Olsson N, Nilsson G. (2002) Selective CCL5/RANTES-induced mast cell migration through interactions with chemokine receptors CCR1 and CCR4. Biochem Biophys Res Commun, 297 (3): 480-5. [PMID:12270118]

19. Kim IS, Jang SW, Sung HJ, Lee JS, Ko J. (2005) Differential CCR1-mediated chemotaxis signaling induced by human CC chemokine HCC-4/CCL16 in HOS cells. FEBS Lett, 579 (27): 6044-8. [PMID:16226254]

20. Kledal TN, Rosenkilde MM, Coulin F, Simmons G, Johnsen AH, Alouani S, Power CA, Lüttichau HR, Gerstoft J, Clapham PR et al.. (1997) A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus. Science, 277 (5332): 1656-9. [PMID:9287217]

21. Ko J, Kim IS, Jang SW, Lee YH, Shin SY, Min DS, Na DS. (2002) Leukotactin-1/CCL15-induced chemotaxis signaling through CCR1 in HOS cells. FEBS Lett, 515 (1-3): 159-64. [PMID:11943214]

22. 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]

23. Li L, Pennell AMK, Zhang P. (2008) 3-(imidazolyl)-pyrazolo[3,4-b]pyridines. Patent number: WO2008147815A1. Assignee: Chemocentryx, Inc.. Priority date: 22/05/2007. Publication date: 04/12/2008.

24. Liang M, Mallari C, Rosser M, Ng HP, May K, Monahan S, Bauman JG, Islam I, Ghannam A, Buckman B et al.. (2000) Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem, 275 (25): 19000-8. [PMID:10748002]

25. Meucci O, Fatatis A, Simen AA, Bushell TJ, Gray PW, Miller RJ. (1998) Chemokines regulate hippocampal neuronal signaling and gp120 neurotoxicity. Proc Natl Acad Sci USA, 95 (24): 14500-5. [PMID:9826729]

26. Mo R, Chen J, Han Y, Bueno-Cannizares C, Misek DE, Lescure PA, Hanash S, Yung RL. (2003) T cell chemokine receptor expression in aging. J Immunol, 170 (2): 895-904. [PMID:12517955]

27. Naya A, Ishikawa M, Matsuda K, Ohwaki K, Saeki T, Noguchi K, Ohtake N. (2003) Structure-activity relationships of xanthene carboxamides, novel CCR1 receptor antagonists. Bioorg Med Chem, 11 (6): 875-84. [PMID:12614873]

28. 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]

29. 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]

30. 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]

31. Santella 3rd JB, Gardner DS, Duncia JV, Wu H, Dhar M, Cavallaro C, Tebben AJ, Carter PH, Barrish JC, Yarde M et al.. (2014) Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis. J Med Chem, 57 (18): 7550-64. [PMID:25101488]

32. Sarau HM, Rush JA, Foley JJ, Brawner ME, Schmidt DB, White JR, Barnette MS. (1997) Characterization of functional chemokine receptors (CCR1 and CCR2) on EoL-3 cells: a model system to examine the role of chemokines in cell function. J Pharmacol Exp Ther, 283 (1): 411-8. [PMID:9336350]

33. Su SB, Mukaida N, Wang J, Nomura H, Matsushima K. (1996) Preparation of specific polyclonal antibodies to a C-C chemokine receptor, CCR1, and determination of CCR1 expression on various types of leukocytes. J Leukoc Biol, 60: 658-666. [PMID:8929558]

34. Topham PS, Csizmadia V, Soler D, Hines D, Gerard CJ, Salant DJ, Hancock WW. (1999) Lack of chemokine receptor CCR1 enhances Th1 responses and glomerular injury during nephrotoxic nephritis. J Clin Invest, 104 (11): 1549-57. [PMID:10587518]

35. 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]

36. Wieser F, Dogan S, Klingel K, Diedrich K, Taylor RN, Hornung D. (2005) Expression and regulation of CCR1 in peritoneal macrophages from women with and without endometriosis. Fertil Steril, 83 (6): 1878-81. [PMID:15950672]

37. 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]

38. Zoffmann S, Turcatti G, Galzi J, Dahl M, Chollet A. (2001) Synthesis and characterization of fluorescent and photoactivatable MIP-1alpha ligands and interactions with chemokine receptors CCR1 and CCR5. J Med Chem, 44 (2): 215-22. [PMID:11170631]

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