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Target intelligence / Profile preview
Complement component C5a receptor 1 (C5aR1)
- Target
- C5aR1
- Molecular classification
- G protein-coupled receptor, GPCR, Class A GPCR
01
Overview
Complement component C5a receptor 1 (C5aR1) is a G protein-coupled receptor that binds the complement fragment peptide C5a. It is primarily expressed on cells involved in innate immunity, such as granulocytes, monocytes, macrophages, and dendritic cells. Activation of C5aR1 by C5a leads to a variety of downstream effects, including chemotaxis, phagocytosis, and cytokine secretion. Dysregulation of C5aR1 signaling can contribute to various diseases, including inflammatory diseases, infectious diseases, cancer, and cardiovascular disease. Several potent agonists and antagonists of C5aR1 have been developed, including avacopan (CCX168) and CHIPS, offering therapeutic potential for inflammatory diseases.
- Other names
- CD88C5AR1Complement component 5a receptor 1C5a anaphylatoxin chemotactic receptor 1
02
Mechanism of action
Antagonism of C5aR1
03
Biological functions
Modulation of inflammatory responsesChemotaxisPhagocytosisCytokine secretionImmune responseSignal transduction
04
Disease associations
Inflammatory diseasesInfectious diseasesCancerCardiovascular diseaseIschemic injuriesChronic kidney diseaseObesityAutoimmune diseases
05
Safety considerations
Excessive immune suppressionPotential for off-target effectsRisk of infection
06
Interacting drugs
Avacopan (CCX168)
1 more in the full profile.
07
Biomarkers
C5a levels in severe COVID-19C5aR1 expression in myeloid-derived suppressor cellsC5aR1 expression in cardiomyocytes after heart injury
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