Contents:
- Gene and Protein Information
- Previous and Unofficial Names
- Database Links
- Natural/Endogenous Ligands
- Rank order lists
- Agonists
- Antagonists
- Immunopharmacology Comments
- Immuno Cell Type Associations
- Immuno Process Associations
- Transduction Mechanisms
- Tissue Distribution
- Expression Datasets
- Functional Assays
- Physiological Functions
- Physiological Consequences of Altering Gene Expression
- Phenotypes, Alleles and Disease Models
- Clinically-Relevant Mutations and Pathophysiology
- References
- Contributors
- How to cite this page
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 | 482 | 12p13.31 | C3AR1 | complement C3a receptor 1 | 24 |
| Mouse | 7 | 477 | 6 F2 | C3ar1 | complement component 3a receptor 1 | 24 |
| Rat | 7 | 473 | 4q42 | C3ar1 | complement C3a receptor 1 | |
| Previous and Unofficial Names |
| C3AR | C3a anaphylatoxin chemotactic receptor | C3a-R | anaphylatoxin C3a receptor | complement component 3a receptor 1 |
| Database Links |
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| Specialist databases | |
| GPCRdb | c3ar_human (Hs), c3ar_mouse (Mm), c3ar_rat (Rn) |
| Other databases | |
| Alphafold | Q16581 (Hs), O09047 (Mm), O55197 (Rn) |
| ChEMBL Target | CHEMBL4761 (Hs) |
| Ensembl Gene | ENSG00000171860 (Hs), ENSMUSG00000040552 (Mm), ENSRNOG00000009211 (Rn) |
| Entrez Gene | 719 (Hs), 12267 (Mm), 84007 (Rn) |
| Human Protein Atlas | ENSG00000171860 (Hs) |
| KEGG Gene | hsa:719 (Hs), mmu:12267 (Mm), rno:84007 (Rn) |
| OMIM | 605246 (Hs) |
| Pharos | Q16581 (Hs) |
| RefSeq Nucleotide | NM_004054 (Hs), NM_009779 (Mm), NM_032060 (Rn) |
| RefSeq Protein | NP_004045 (Hs), NP_033909 (Mm), NP_114449 (Rn) |
| UniProtKB | Q16581 (Hs), O09047 (Mm), O55197 (Rn) |
| Wikipedia | C3AR1 (Hs) |
| Natural/Endogenous Ligands |
| C5a {Sp: Human} |
| C3a {Sp: Human} |
| C5a {Sp: Mouse} |
| C3a {Sp: Mouse} |
| C5a {Sp: Rat} |
| C3a {Sp: Rat} |
| Comments: C3a anaphylatoxin has a higher potency than C5a anaphylatoxin |
| Potency order of endogenous ligands (Human) |
| C3a (C3, P01024) > C5a (C5, P01031) [3] |
Download all structure-activity data for this target as a CSV file 
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| Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| The receptor affinity of pEC50 5.9 for WWGKKYRASKLGLAR was detected by a binding assay. C3a receptor has no detectable affinity for the metabolite C3a des Arg. The rodent receptor was recently suggested to interact with vgf gene product TLQP-21, however the binding affinity was found to be relatively low [21]. SB290157 has also been reported to have agonist properties at the C3a receptor [32]. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| The pIC50 value for FLTChaAR affinity value was obtained from a binding assay. SB290157 has also been reported to have agonist properties at the C3a receptor [32]. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Immunopharmacology Comments |
| Complement C3a receptor 1 is the receptor for complement factor C3a, a component of the alternative complement cascade. It can have pro-inflammatory actions, but can also counteract the proinflammatory effects of C5a. The complement system plays a critical role intestinal immune homeostasis. In particular, C3 and the C3aR have been identified as being involved in regulating the intestinal immune response during chronic colitis [48,55]. C3aR is also reported to provide protection from tissue damage in an intestinal ischemia-reperfusion model, an effect that is mediated by inhibition of neutrophil mobilisation [57]. The biological action of C3aR agonists and antagonists can be monitored by measuring receptor-mediated cytokine release from human macrophages [40], and C3aR biology further examined by assessing granulocyte/neutrophil mobilisation in response to injury or G-CSF [57]. |
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| Primary Transduction Mechanisms
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| Transducer | Effector/Response |
| G protein (identity unknown) | Other - See Comments |
| Comments: β-arrestin is required for mast cell degranulation in response to C3a | |
| References: 19,54 | |
| Secondary Transduction Mechanisms |
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| Comments: C3aR exhibits a cell-type specific use of secondary signalling cascades. For example, in astrocytes, C3aR causes a transient increase in intracellular calcium mediated by PKC activity, a decrease in cAMP concentrations and an increase in MAPK pathway constituent phosphorylation [43]. In mast cells and human umbilical vein endothelial cells, C3aR activation has also been shown to cause sustained MAPK phosphorylation, leading to the production of cytokines, however in neural precursors C3aR is an inhibitor of this pathway [33,46,53]. | |
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| Tissue Distribution
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| Expression Datasets |
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| Phenotypes, Alleles and Disease Models
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References
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32. Mathieu MC, Sawyer N, Greig GM, Hamel M, Kargman S, Ducharme Y, Lau CK, Friesen RW, O'Neill GP, Gervais FG et al.. (2005) The C3a receptor antagonist SB 290157 has agonist activity. Immunol Lett, 100 (2): 139-45. [PMID:16154494]
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34. Niebuhr M, Bäumer W, Kietzmann M, Wichmann K, Heratizadeh A, Werfel T. (2012) Participation of complement 3a receptor (C3aR) in the sensitization phase of Th2 mediated allergic contact dermatitis. Exp Dermatol, 21 (1): 52-6. [PMID:22151392]
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