C5a anaphylatoxin chemotactic receptor 1

UniProt P21730 Organism Homo sapiens Gene C5AR, C5AR1, C5R1

Also known as: C5AR, C5AR1, C5R1

Function

Receptor for the chemotactic and inflammatory peptide anaphylatoxin C5a, stimulating chemotaxis, granule enzyme release, intracellular calcium release and superoxide anion production. 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. C5AR1 is coupled to G(i)/G(o) (GNAI1 or GNAO1) G alpha proteins and mediates inhibition of adenylate cyclase. 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.

Classification

Family (Pfam): PF00001 7tm_1
InterPro: Anphylx_rcpt_C3a/C5a1-2, Formyl_rcpt-rel, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
Functional cluster: G Protein-Coupled Receptors

Experimental structures · PDB · 19

2K3U NMR
5O9H X-ray 2.70A
6C1Q X-ray 2.90A
6C1R X-ray 2.20A
7Y64 EM 2.90A
7Y65 EM 3.20A
7Y66 EM 2.90A
7Y67 EM 2.80A
8GO8 EM 3.41A
8GOO EM 4.40A
8HK5 EM 3.00A
8I0N EM 3.26A
… and 7 more

A predicted model is available from AlphaFold.

Gene Ontology · 29

Drugs targeting this protein · 1

AVACOPAN antagonist

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Chemotaxis inhibitory protein 2 shared papers
Complement C5 5 shared papers
C5a anaphylatoxin chemotactic receptor 1 1 shared papers
G protein-coupled receptor kinase 3 1 shared papers
C3a anaphylatoxin chemotactic receptor 3 shared papers
C5a anaphylatoxin chemotactic receptor 1 1 shared papers
N-formyl peptide receptor 1 1 shared papers
G protein-coupled receptor kinase 2 1 shared papers
Complement C3 2 shared papers
Beta-arrestin-1 2 shared papers
Beta-arrestin-2 1 shared papers
Muscarinic acetylcholine receptor M2 1 shared papers

Literature · 24 cited papers

Molecular basis of anaphylatoxin binding, activation, and signaling bias at complement receptors. Cell · 2023
Structural snapshots uncover a key phosphorylation motif in GPCRs driving beta-arrestin activation. Mol. Cell · 2023
Revealing the signaling of complement receptors C3aR and C5aR1 by anaphylatoxins. Nat. Chem. Biol. · 2023
Mechanism of activation and biased signaling in complement receptor C5aR1. Cell Res. · 2023
Orthosteric and allosteric action of the C5a receptor antagonists. Nat. Struct. Mol. Biol. · 2018
Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727. Nature · 2018
Tyrosine sulfation in N-terminal domain of human C5a receptor is necessary for binding of chemotaxis inhibitory protein of Staphylococcus aureus. Acta Pharmacol. Sin. · 2011
Structure of the tyrosine-sulfated C5a receptor N terminus in complex with chemotaxis inhibitory protein of Staphylococcus aureus. J. Biol. Chem. · 2009
Residues 10-18 within the C5a receptor N terminus compose a binding domain for chemotaxis inhibitory protein of Staphylococcus aureus. J. Biol. Chem. · 2005
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
Chemotaxis inhibitory protein of Staphylococcus aureus binds specifically to the C5a and formylated peptide receptor. J. Immunol. · 2004
The DNA sequence and biology of human chromosome 19. Nature · 2004
… and 12 more in the literature graph

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