The C3a receptor also known as complement component 3a receptor 1 (C3AR1) is a G protein-coupled receptor protein involved in the complement system.[5][6]

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.[7] C3a receptor modulates immunity,[8] arthritis, diet-induced obesity[9] and cancers.[10]

Agonists and antagonists

Potent and selective agonists[11] and antagonists[12] for C3aR have been discovered.

References

  1. ^ abcGRCh38: Ensembl release 89: ENSG00000171860 – Ensembl, May 2017
  2. ^ abcGRCm38: Ensembl release 89: ENSMUSG00000040552 – Ensembl, May 2017
  3. ^"Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^"Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^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 (BBA) - Gene Structure and Expression. 1305 (1–2): 39–43. doi:10.1016/0167-4781(95)00209-x. PMID 8605247.
  6. ^Ali H, Panettieri RA (February 2005). "Anaphylatoxin C3a receptors in asthma". Respiratory Research. 6 (1): 19. doi:10.1186/1465-9921-6-19. PMC 551592. PMID 15723703.
  7. ^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.
  8. ^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.
  9. ^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. S2CID 25562647.
  10. ^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.
  11. ^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. Bibcode:2013NatCo...4.2802R. doi:10.1038/ncomms3802. PMID 24257095.
  12. ^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