Recombinant Human C5a-R protein

Specifications

Form

Lyophilized

General info

Function

Receptor for the chemotactic and inflammatory peptide anaphylatoxin C5a, stimulating chemotaxis, granule enzyme release, intracellular calcium release and superoxide anion production (PubMed : 10636859, PubMed : 15153520, PubMed : 1847994, PubMed : 29300009, PubMed : 36806352, PubMed : 7622471, PubMed : 8182049, PubMed : 9553099). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase (PubMed : 36806352, PubMed : 37852260). C5AR1 is coupled to G(i)/G(o) (GNAI1 or GNAO1) G alpha proteins and mediates inhibition of adenylate cyclase (PubMed : 36806352, PubMed : 37852260). The ligand interacts with at least two sites on the receptor : a high-affinity site on the extracellular N-terminus, and a second site in the transmembrane region which activates downstream signaling events (PubMed : 7622471, PubMed : 8182049, PubMed : 9553099).

Sequence similarities

Belongs to the G-protein coupled receptor 1 family.

Post-translational modifications

Phosphorylation of the P-X-P-P motif by GRK2 or GRK3 in response to C5a binding promotes association with beta-arrestin (ARRB1 and/or ARRB2), resulting in internalization of the receptor and short-term desensitization to the ligand.. Sulfation plays a critical role in the association of C5aR with C5a, but no significant role in the ability of the receptor to transduce a signal and mobilize calcium in response to a small a small peptide agonist (PubMed:11342590). Sulfation at Tyr-14 is important for CHIPS binding (PubMed:21706042).