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Gene and Protein Information  |
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| class A G protein-coupled receptor | ||||||
| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 7 | 374 | 3p21.31 | CCR2 | C-C motif chemokine receptor 2 | 18,67 |
| Mouse | 7 | 373 | 9 75.05 cM | Ccr2 | C-C motif chemokine receptor 2 | 44,51 |
| Rat | 7 | 373 | 8q32 | Ccr2 | C-C motif chemokine receptor 2 | 7,38 |
| Previous and Unofficial Names |
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| MCP-1 receptor [18,30] | CC CKR2 | CKR2 | CD192 | chemokine receptor CCR2 | CCR2A | CCR2B | chemokine (C-C motif) receptor 2 | |
| Database Links |
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| Specialist databases | |
| GPCRdb | ccr2_human (Hs), ccr2_mouse (Mm), ccr2_rat (Rn) |
| Other databases | |
| Alphafold | P41597 (Hs), P51683 (Mm), O55193 (Rn) |
| ChEMBL Target | CHEMBL4015 (Hs), CHEMBL5412 (Mm), CHEMBL1293204 (Rn) |
| Ensembl Gene | ENSG00000121807 (Hs), ENSMUSG00000049103 (Mm), ENSRNOG00000063127 (Rn) |
| Entrez Gene | 1231 (Hs), 12772 (Mm), 60463 (Rn) |
| Human Protein Atlas | ENSG00000121807 (Hs) |
| KEGG Gene | hsa:1231 (Hs), mmu:12772 (Mm), rno:60463 (Rn) |
| OMIM | 601267 (Hs) |
| Pharos | P41597 (Hs) |
| RefSeq Nucleotide | NM_001123396 (Hs), NM_009915 (Mm), NM_021866 (Rn) |
| RefSeq Protein | NP_001116513 (Hs), NP_001116868 (Hs), NP_034045 (Mm), NP_068638 (Rn) |
| SynPHARM |
84094 (in complex with BMS-681) 84096 (in complex with CCR2-RA-[R]) |
| UniProtKB | P41597 (Hs), P51683 (Mm), O55193 (Rn) |
| Wikipedia | CCR2 (Hs) |
| Selected 3D Structures |
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| Natural/Endogenous Ligands |
| CCL24 {Sp: Human} |
| CCL7 {Sp: Human} |
| CCL13 {Sp: Human} |
| CCL2 {Sp: Human} |
| CCL8 {Sp: Human} |
| CCL16 {Sp: Human} |
| CCL11 {Sp: Human} |
| CCL26 {Sp: Human} |
| CCL2 {Sp: Mouse} |
| CCL7 {Sp: Mouse} |
| CCL8 {Sp: Mouse} |
| CCL11 {Sp: Mouse} |
| CCL2 {Sp: Rat} |
| CCL7 {Sp: Rat} |
| CCL11 {Sp: Rat} |
| Comments: CCL2 is the principal endogenous agonist |
Download all structure-activity data for this target as a CSV file 
| Agonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| It has been shown that CCL12 is a ligand for the CCR2 receptor [69]. vCCL4 is the secreted protein product of the U83 gene from the human herpesvirus 6 [49]. |
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| Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| View species-specific antagonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Allosteric Modulators | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Antibodies | |||||||||||||||||||||||||||||||||||||||||||||||||||
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| Immunopharmacology Comments |
| CCR2 is one of more than 20 distinct chemokine receptors expressed in human leukocytes. Chemokines primarily act to promote leukocyte chemotaxis to sites of inflammation. CCR2 is discussed in relation to immuno-oncology in [2]. |
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| Primary Transduction Mechanisms
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| Transducer | Effector/Response |
| Gi/Go family | |
| References: 39 | |
| Tissue Distribution
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| Expression Datasets |
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| Functional Assays
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| Physiological Functions
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| Physiological Consequences of Altering Gene Expression
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| Phenotypes, Alleles and Disease Models
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| Clinically-Relevant Mutations and Pathophysiology
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1. Abbadie C, Lindia JA, Cumiskey AM, Peterson LB, Mudgett JS, Bayne EK, DeMartino JA, MacIntyre DE, Forrest MJ. (2003) Impaired neuropathic pain responses in mice lacking the chemokine receptor CCR2. Proc Natl Acad Sci USA, 100 (13): 7947-52. [PMID:12808141]
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13. Boring L, Gosling J, Cleary M, Charo IF. (1998) Decreased lesion formation in CCR2-/- mice reveals a role for chemokines in the initiation of atherosclerosis. Nature, 394 (6696): 894-7. [PMID:9732872]
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16. Campbell EM, Charo IF, Kunkel SL, Strieter RM, Boring L, Gosling J, Lukacs NW. (1999) Monocyte chemoattractant protein-1 mediates cockroach allergen-induced bronchial hyperreactivity in normal but not CCR2-/- mice: the role of mast cells. J Immunol, 163 (4): 2160-7. [PMID:10438957]
17. Carter PH, Brown GD, Cherney RJ, Batt DG, Chen J, Clark CM, Cvijic ME, Duncia JV, Ko SS, Mandlekar S et al.. (2015) Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5. ACS Med Chem Lett, 6 (4): 439-44. [PMID:25893046]
18. Charo IF, Myers SJ, Herman A, Franci C, Connolly AJ, Coughlin SR. (1994) Molecular cloning and functional expression of two monocyte chemoattractant protein 1 receptors reveals alternative splicing of the carboxyl-terminal tails. Proc Natl Acad Sci USA, 91 (7): 2752-6. [PMID:8146186]
19. Chiu BC, Freeman CM, Stolberg VR, Hu JS, Zeibecoglou K, Lu B, Gerard C, Charo IF, Lira SA, Chensue SW. (2004) Impaired lung dendritic cell activation in CCR2 knockout mice. Am J Pathol, 165 (4): 1199-209. [PMID:15466386]
20. Coelho A, Matos A, Catarino R, Pinto D, Pereira D, Lopes C, Medeiros R. (2005) Protective role of the polymorphism CCR2-64I in the progression from squamous intraepithelial lesions to invasive cervical carcinoma. Gynecol Oncol, 96 (3): 760-4. [PMID:15721423]
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31. Held KS, Chen BP, Kuziel WA, Rollins BJ, Lane TE. (2004) Differential roles of CCL2 and CCR2 in host defense to coronavirus infection. Virology, 329 (2): 251-60. [PMID:15518805]
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35. 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]
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37. Jarnagin K, Grunberger D, Mulkins M, Wong B, Hemmerich S, Paavola C, Bloom A, Bhakta S, Diehl F, Freedman R et al.. (1999) Identification of surface residues of the monocyte chemotactic protein 1 that affect signaling through the receptor CCR2. Biochemistry, 38 (49): 16167-77. [PMID:10587439]
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target has curated data in GtoImmuPdb
