C5AR1

Synonyms

Receptor, Anaphylatoxin C5a, C5a-R, Complement Component 5 Receptor 1 (C5a Ligand), C5a Anaphylatoxin Chemotactic Receptor, C5AR, Complement C5a Receptor 1, Complement Component 5a Receptor 1, C5a Anaphylatoxin Chemotactic Receptor 1, C5a Anaphylatoxin Receptor, C5AR1, C5R1, C5A, CD88, C5a Ligand, CD88 Antigen, Complement Component 5 Receptor 1

Description

Receptor for the chemotactic and inflammatory peptide anaphylatoxin C5a . 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 . Receptor activation stimulates chemotaxis, granule enzyme release, intracellular calcium release and superoxide anion production .

KO Status

Immunization

Drug Information

Drugs in clinical trials: 2
Latest Research Phase: Phase 3 Clinical

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Avacopan

CCX-168

Phase 3 Clinical

Chemocentryx

Anti-Neutrophil Cytoplasmic Antibody-Associated Vasculitis, Glomerulonephritis, IGA, Vasculitis, Glomerulonephritis, Membranoproliferative, Hidradenitis Suppurativa

Avdoralimab

NN-8210, IPH-5401, Anti-C5aR-215, NNC-0215-0384

Phase 2 Clinical

Novo Nordisk A/S

Neoplasms, Arthritis, Rheumatoid, Coronavirus Disease 2019 (COVID-19), Inflammation

PMX-53

PMX-53

Discontinued

Cephalon

Arthritis, Rheumatoid, Psoriasis, Osteoarthritis

NGD-2000-1

NGD-2000-1, NDT-9509589

Discontinued

Arthritis, Rheumatoid, Asthma

EP-67

EP-67

Discontinued

Prommune

Asthma

MP-435

MP-435

Discontinued

Mitsubishi Tanabe Pharma Corp

Arthritis, Rheumatoid

MEDI-7814

MEDI-7814

Discontinued

Medimmune

Pulmonary Disease, Chronic Obstructive

References


Title

Authors

Source

C5a receptor oligomerization. I. Disulfide trapping reveals oligomers and potential contact surfaces in a G protein-coupled receptor

Klco J.M., Lassere T.B., Baranski T.J.,

J. Biol. Chem. 278:35345-35353(2003)

Chemotaxis inhibitory protein of Staphylococcus aureus binds specifically to the C5a and formylated peptide receptor

Postma B., Poppelier M.J.J.G., van Galen J.C., Prossnitz E.R., van Strijp J.A.G., de Haas C.J.C., van Kessel K.P.M.,

J. Immunol. 172:6994-7001(2004)

Residues 10-18 within the C5a receptor N terminus compose a binding domain for chemotaxis inhibitory protein of Staphylococcus aureus

Postma B., Kleibeuker W., Poppelier M.J.J.G., Boonstra M., van Kessel K.P.M., van Strijp J.A.G., de Haas C.J.C.,

J. Biol. Chem. 280:2020-2027(2005)

Tyrosine sulfation in N-terminal domain of human C5a receptor is necessary for binding of chemotaxis inhibitory protein of Staphylococcus aureus

Liu Z.J., Yang Y.J., Jiang L., Xu Y.C., Wang A.X., Du G.H., Gao J.M.,

Acta Pharmacol. Sin. 32:1038-1044(2011)

Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727

Robertson N., Rappas M., Dore A.S., Brown J., Bottegoni G., Koglin M., Cansfield J., Jazayeri A., Cooke R.M., Marshall F.H.,

Nature 553:111-114(2018)

Expression cloning of a receptor for C5a anaphylatoxin on differentiated HL-60 cells

Boulay F., Mery L., Tardif M., Brouchon L., Vignais P.,

Biochemistry 30:2993-2999(1991)

The chemotactic receptor for human C5a anaphylatoxin

Gerard N.P., Gerard C.,

Nature 349:614-617(1991)

Human chemotaxis receptor genes cluster at 19q13.3-13.4. Characterization of the human C5a receptor gene

Gerard N.P., Bao L., Xiao-Ping H., Eddy R.L. Jr., Shows T.B., Gerard C.,

Biochemistry 32:1243-1250(1993)

The amino terminus of the human C5a receptor is required for high affinity C5a binding and for receptor activation by C5a but not C5a analogs

DeMartino J.A., Van Riper G., Siciliano S.J., Molineaux C.J., Konteatis Z.D., Rosen H., Springer M.S.,

J. Biol. Chem. 269:14446-14450(1994)

Mutation of glutamate 199 of the human C5a receptor defines a binding site for ligand distinct from the receptor N terminus

Monk P.N., Barker M.D., Partridge L.J., Pease J.E.,

J. Biol. Chem. 270:16625-16629(1995)