Target intelligence / Profile preview

Complement component C5a

Molecular classification: Anaphylatoxin, Chemotactic factor, Complement component

Overview

Complement component C5a is a potent, 74-amino acid glycoprotein fragment (~11 kDa) generated by the enzymatic cleavage of complement component C5 by C5 convertase. It acts as a highly inflammatory peptide with multiple roles in immune regulation and inflammation, functioning as both an anaphylatoxin and a chemotactic agent.

Mechanism of action

C5a exerts its effects primarily through binding two G protein-coupled receptors: C5aR1 (CD88) and C5L2 (GPR77), triggering intracellular signaling cascades involving G proteins, β-arrestin recruitment, ERK1/2 phosphorylation, and calcium mobilization.

Biological functions

AnaphylaxisChemotaxisInflammationImmune modulationCytokine productionLeukocyte activation

Disease associations

SepsisAcute lung injuryIschemia-reperfusion injuryAsthmaInflammatory diseasesTumor progression

Safety considerations

Excessive or dysregulated production/activity of C5a has been implicated in numerous acute/chronic inflammatory diseases.High levels within tumor microenvironments may suppress anti-tumor T-cell responses.

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