C5aR2 agonist – Other Categories

C5a receptor 2 (C5aR2, or C5L2) is a seven transmembrane non-G-protein-signalling receptor which binds the complement activation peptide C5a ligand. The complement cascade is a highly sophisticated network of innate immune proteins that are activated in response to invading pathogens or tissue injury. C5aR2 regulates the release of certain cytokines and is involved in a number of inflammatory conditions. C5aR2 can recruit and form a complex with β-arrestins, which can modulate ERK1/2 signalling in macrophages and neutrophils. C5aR2 has both pro- and anti-inflammatory actions. P32 is a functionally selective C5aR2 ligand which is able to recruit β-arrestin 2 with high efficacy, inhibit C5a-induced ERK1/2 activation and can selectively inhibit LPS-induced IL-6 release from human monocyte-derived macrophages (HMDMs). Functionally selective ligands for C5aR2 such as this are novel tools that can selectively modulate C5a activity and are therefore valuable tools in investigating C5aR2 function.