C3a receptor

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RefSeq (mRNA)



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The C3a receptor also known as complement component 3a receptor 1 (C3AR1) is a G protein-coupled receptor protein involved in the complement system.[1][2]

The receptor binds to complement component C3a, although there is limited evidence that this receptor also binds C4a in lesser mammals this has yet to be proven true in humans.[3] C3a receptor modulates immunity,[4] arthritis, diet-induced obesity[5] and cancers[6]

Agonists and antagonists

Potent and selective agonists[7] and antagonists[8] for C3aR have been discovered.


  1. Roglic A, Prossnitz ER, Cavanagh SL, Pan Z, Zou A, Ye RD (February 1996). "cDNA cloning of a novel G protein-coupled receptor with a large extracellular loop structure". Biochimica et Biophysica Acta. 1305 (1–2): 39–43. doi:10.1016/0167-4781(95)00209-x. PMID 8605247.
  2. Ali H, Panettieri RA (February 2005). "Anaphylatoxin C3a receptors in asthma". Respiratory Research. 6: 19. doi:10.1186/1465-9921-6-19. PMC 551592. PMID 15723703.
  3. Klos A, Wende E, Wareham KJ, Monk PN (January 2013). "International Union of Basic and Clinical Pharmacology. [corrected]. LXXXVII. Complement peptide C5a, C4a, and C3a receptors". Pharmacological Reviews. 65 (1): 500–43. doi:10.1124/pr.111.005223. PMID 23383423.
  4. Cravedi P, Leventhal J, Lakhani P, Ward SC, Donovan MJ, Heeger PS (October 2013). "Immune cell-derived C3a and C5a costimulate human T cell alloimmunity". American Journal of Transplantation. 13 (10): 2530–9. doi:10.1111/ajt.12405. PMC 3809075. PMID 24033923.
  5. Lim J, Iyer A, Suen JY, Seow V, Reid RC, Brown L, Fairlie DP (February 2013). "C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling". FASEB Journal. 27 (2): 822–31. doi:10.1096/fj.12-220582. PMID 23118029.
  6. Sayegh ET, Bloch O, Parsa AT (August 2014). "Complement anaphylatoxins as immune regulators in cancer". Cancer Medicine. 3 (4): 747–58. doi:10.1002/cam4.241. PMC 4303144. PMID 24711204.
  7. Reid RC, Yau MK, Singh R, Hamidon JK, Reed AN, Chu P, Suen JY, Stoermer MJ, Blakeney JS, Lim J, Faber JM, Fairlie DP (2013). "Downsizing a human inflammatory protein to a small molecule with equal potency and functionality". Nature Communications. 4: 2802. doi:10.1038/ncomms3802. PMID 24257095.
  8. Reid RC, Yau MK, Singh R, Lim J, Fairlie DP (August 2014). "Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides". Journal of the American Chemical Society. 136 (34): 11914–7. doi:10.1021/ja506518t. PMID 25102224.

Further reading

  • Sim RB, Laich A (October 2000). "Serine proteases of the complement system". Biochemical Society Transactions. 28 (5): 545–50. doi:10.1042/bst0280545. PMID 11044372.
  • Maruyama K, Sugano S (January 1994). "Oligo-capping: a simple method to replace the cap structure of eukaryotic mRNAs with oligoribonucleotides". Gene. 138 (1–2): 171–4. doi:10.1016/0378-1119(94)90802-8. PMID 8125298.
  • Roglic A, Prossnitz ER, Cavanagh SL, Pan Z, Zou A, Ye RD (February 1996). "cDNA cloning of a novel G protein-coupled receptor with a large extracellular loop structure". Biochimica et Biophysica Acta. 1305 (1–2): 39–43. doi:10.1016/0167-4781(95)00209-x. PMID 8605247.
  • Ames RS, Li Y, Sarau HM, Nuthulaganti P, Foley JJ, Ellis C, Zeng Z, Su K, Jurewicz AJ, Hertzberg RP, Bergsma DJ, Kumar C (August 1996). "Molecular cloning and characterization of the human anaphylatoxin C3a receptor". The Journal of Biological Chemistry. 271 (34): 20231–4. doi:10.1074/jbc.271.34.20231. PMID 8702752.
  • Crass T, Raffetseder U, Martin U, Grove M, Klos A, Köhl J, Bautsch W (August 1996). "Expression cloning of the human C3a anaphylatoxin receptor (C3aR) from differentiated U-937 cells". European Journal of Immunology. 26 (8): 1944–50. doi:10.1002/eji.1830260840. PMID 8765043.
  • Ames RS, Nuthulaganti P, Kumar C (October 1996). "In Xenopus oocytes the human C3a and C5a receptors elicit a promiscuous response to the anaphylatoxins". FEBS Letters. 395 (2–3): 157–9. doi:10.1016/0014-5793(96)01018-6. PMID 8898085.
  • Martin U, Bock D, Arseniev L, Tornetta MA, Ames RS, Bautsch W, Köhl J, Ganser A, Klos A (July 1997). "The human C3a receptor is expressed on neutrophils and monocytes, but not on B or T lymphocytes". The Journal of Experimental Medicine. 186 (2): 199–207. doi:10.1084/jem.186.2.199. PMC 2198980. PMID 9221749.
  • Suzuki Y, Yoshitomo-Nakagawa K, Maruyama K, Suyama A, Sugano S (October 1997). "Construction and characterization of a full length-enriched and a 5'-end-enriched cDNA library". Gene. 200 (1–2): 149–56. doi:10.1016/S0378-1119(97)00411-3. PMID 9373149.
  • Hollmann TJ, Haviland DL, Kildsgaard J, Watts K, Wetsel RA (February 1998). "Cloning, expression, sequence determination, and chromosome localization of the mouse complement C3a anaphylatoxin receptor gene". Molecular Immunology. 35 (3): 137–48. doi:10.1016/S0161-5890(98)00021-2. PMID 9694514.
  • Lienenklaus S, Ames RS, Tornetta MA, Sarau HM, Foley JJ, Crass T, Sohns B, Raffetseder U, Grove M, Hölzer A, Klos A, Köhl J, Bautsch W (September 1998). "Human anaphylatoxin C4a is a potent agonist of the guinea pig but not the human C3a receptor". Journal of Immunology. 161 (5): 2089–93. PMID 9725198.
  • Davoust N, Jones J, Stahel PF, Ames RS, Barnum SR (May 1999). "Receptor for the C3a anaphylatoxin is expressed by neurons and glial cells". Glia. 26 (3): 201–11. doi:10.1002/(SICI)1098-1136(199905)26:3<201::AID-GLIA2>3.0.CO;2-M. PMID 10340761.
  • Settmacher B, Bock D, Saad H, Gärtner S, Rheinheimer C, Köhl J, Bautsch W, Klos A (June 1999). "Modulation of C3a activity: internalization of the human C3a receptor and its inhibition by C5a". Journal of Immunology. 162 (12): 7409–16. PMID 10358194.
  • Feild JA, Foley JJ, Testa TT, Nuthulaganti P, Ellis C, Sarau HM, Ames RS (October 1999). "Cloning and characterization of a rabbit ortholog of human Galpha16 and mouse G(alpha)15". FEBS Letters. 460 (1): 53–6. doi:10.1016/S0014-5793(99)01317-4. PMID 10571060.
  • Petering H, Köhl J, Weyergraf A, Dulkys Y, Kimmig D, Smolarski R, Kapp A, Elsner J (April 2000). "Characterization of synthetic C3a analog peptides on human eosinophils in comparison to the native complement component C3a". Journal of Immunology. 164 (7): 3783–9. doi:10.4049/jimmunol.164.7.3783. PMID 10725738.
  • Drouin SM, Kildsgaard J, Haviland J, Zabner J, Jia HP, McCray PB, Tack BF, Wetsel RA (February 2001). "Expression of the complement anaphylatoxin C3a and C5a receptors on bronchial epithelial and smooth muscle cells in models of sepsis and asthma". Journal of Immunology. 166 (3): 2025–32. doi:10.4049/jimmunol.166.3.2025. PMID 11160252.
  • Ames RS, Lee D, Foley JJ, Jurewicz AJ, Tornetta MA, Bautsch W, Settmacher B, Klos A, Erhard KF, Cousins RD, Sulpizio AC, Hieble JP, McCafferty G, Ward KW, Adams JL, Bondinell WE, Underwood DC, Osborn RR, Badger AM, Sarau HM (May 2001). "Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models". Journal of Immunology. 166 (10): 6341–8. doi:10.4049/jimmunol.166.10.6341. PMID 11342658.
  • Kirchhoff K, Weinmann O, Zwirner J, Begemann G, Götze O, Kapp A, Werfel T (June 2001). "Detection of anaphylatoxin receptors on CD83+ dendritic cells derived from human skin". Immunology. 103 (2): 210–7. doi:10.1046/j.1365-2567.2001.01197.x. PMC 1783227. PMID 11412308.
  • Reca R, Mastellos D, Majka M, Marquez L, Ratajczak J, Franchini S, Glodek A, Honczarenko M, Spruce LA, Janowska-Wieczorek A, Lambris JD, Ratajczak MZ (May 2003). "Functional receptor for C3a anaphylatoxin is expressed by normal hematopoietic stem/progenitor cells, and C3a enhances their homing-related responses to SDF-1". Blood. 101 (10): 3784–93. doi:10.1182/blood-2002-10-3233. PMID 12511407.

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