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C5AR1 is a G protein-coupled receptor (GPCR) that serves as the primary receptor for the complement anaphylatoxin C5a. It plays a central role in mediating inflammatory and immune responses. Upon binding to C5a, it stimulates chemotaxis of phagocytic cells, induces granule enzyme release, and triggers superoxide anion production. Dysregulated activation of C5AR1 contributes to pathological inflammation. Antagonists are being developed for anti-inflammatory therapies.
Orthosteric and allosteric antagonism
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