Biology:C5a receptor

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Short description: Mammalian protein found in Homo sapiens


A representation of the 3D structure of the protein myoglobin showing turquoise α-helices.
Generic protein structure example


The C5a receptor also known as complement component 5a receptor 1 (C5AR1) or CD88 (Cluster of Differentiation 88) is a G protein-coupled receptor for C5a. It functions as a complement receptor.[1] C5a receptor modulates inflammatory responses, obesity, development and cancers.[2][3][4]

C5a receptor structure and its residues possessing role in ligand binding or signaling.

Cells

The C5a receptor is expressed on:[5]

  • Granulocytes
  • Monocytes
  • Dendritic cells
  • Hepatoma-derived cell line HepG2
  • Astrocytes
  • Microglia

Agonist and antagonists

Potent and selective agonist and antagonists for C5aR have been developed.[6][7][8][9][10][11]

See also

References

  1. ↑ "C5A anaphylatoxin and its seven transmembrane-segment receptor". Annual Review of Immunology 12: 775–808. 1994. doi:10.1146/annurev.iy.12.040194.004015. PMID 8011297. 
  2. ↑ "The Complement Receptor C5aR Controls Acute Inflammation and Astrogliosis following Spinal Cord Injury". The Journal of Neuroscience 35 (16): 6517–31. April 2015. doi:10.1523/JNEUROSCI.5218-14.2015. PMID 25904802. 
  3. ↑ "C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling". FASEB Journal 27 (2): 822–31. February 2013. doi:10.1096/fj.12-220582. PMID 23118029. 
  4. ↑ "Modulation of the antitumor immune response by complement". Nature Immunology 9 (11): 1225–35. November 2008. doi:10.1038/ni.1655. PMID 18820683. 
  5. ↑ "International Union of Basic and Clinical Pharmacology. [corrected]. LXXXVII. Complement peptide C5a, C4a, and C3a receptors". Pharmacological Reviews 65 (1): 500–43. January 2013. doi:10.1124/pr.111.005223. PMID 23383423. 
  6. ↑ Gorman, Declan M.; Li, Xaria X.; Lee, John D.; Fung, Jenny N.; Cui, Cedric S.; Lee, Han Siean; Rolfe, Barbara E.; Woodruff, Trent M. et al. (2021-11-25). "Development of Potent and Selective Agonists for Complement C5a Receptor 1 with In Vivo Activity" (in en). Journal of Medicinal Chemistry 64 (22): 16598–16608. doi:10.1021/acs.jmedchem.1c01174. ISSN 0022-2623. PMID 34762432. https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01174. 
  7. ↑ "Small molecular probes for G-protein-coupled C5a receptors: conformationally constrained antagonists derived from the C terminus of the human plasma protein C5a". Journal of Medicinal Chemistry 41 (18): 3417–25. August 1998. doi:10.1021/jm9800651. PMID 9719594. 
  8. ↑ "Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists". Bioorganic & Medicinal Chemistry Letters 18 (14): 3852–5. July 2008. doi:10.1016/j.bmcl.2008.06.059. PMID 18595693. 
  9. ↑ "Identification of a potent and orally active non-peptide C5a receptor antagonist". The Journal of Biological Chemistry 277 (51): 49403–7. December 2002. doi:10.1074/jbc.M209672200. PMID 12384495. 
  10. ↑ "Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists". Scientific Reports 6 (1): 24575. April 2016. doi:10.1038/srep24575. PMID 27094554. Bibcode: 2016NatSR...624575S. 
  11. ↑ Ulrich, J. T.; Cieplak, W.; Paczkowski, N. J.; Taylor, S. M.; Sanderson, S. D. (2000). "Induction of an antigen-specific CTL response by a conformationally biased agonist of human C5a anaphylatoxin as a molecular adjuvant". Journal of Immunology (Baltimore, Md. : 1950) 164 (10): 5492–5498. doi:10.4049/jimmunol.164.10.5492. PMID 10799917. 

Further reading

  • "Complement receptors in neutrophils". Critical Reviews in Immunology 15 (2): 107–31. 1996. doi:10.1615/critrevimmunol.v15.i2.10. PMID 8573284. 
  • "Mast cell granule composition and tissue location--a close correlation". Histology and Histopathology 15 (3): 937–46. July 2000. PMID 10963136. 
  • "Roles of the ribosomal protein S19 dimer and the C5a receptor in pathophysiological functions of phagocytic leukocytes". Pathology International 57 (1): 1–11. January 2007. doi:10.1111/j.1440-1827.2007.02049.x. PMID 17199736. 
  • "Mapping of genes for the human C5a receptor (C5AR), human FMLP receptor (FPR), and two FMLP receptor homologue orphan receptors (FPRH1, FPRH2) to chromosome 19". Genomics 13 (2): 437–40. June 1992. doi:10.1016/0888-7543(92)90265-T. PMID 1612600. 
  • "The chemotactic receptor for human C5a anaphylatoxin". Nature 349 (6310): 614–7. February 1991. doi:10.1038/349614a0. PMID 1847994. Bibcode: 1991Natur.349..614G. 
  • "Expression cloning of a receptor for C5a anaphylatoxin on differentiated HL-60 cells". Biochemistry 30 (12): 2993–9. March 1991. doi:10.1021/bi00226a002. PMID 2007135. 
  • "HIV-1 and its envelope glycoprotein down-regulate chemotactic ligand receptors and chemotactic function of peripheral blood monocytes". Journal of Immunology 142 (10): 3553–9. May 1989. PMID 2541200. 
  • "C5a-induced expression of P-selectin in endothelial cells". The Journal of Clinical Investigation 94 (3): 1147–55. September 1994. doi:10.1172/JCI117430. PMID 7521884. 
  • "Identification of the major phosphorylation sites in human C5a anaphylatoxin receptor in vivo". The Journal of Biological Chemistry 270 (32): 19166–72. August 1995. doi:10.1074/jbc.270.32.19166. PMID 7642584. 
  • "Mitogen-activated protein kinase activation requires two signal inputs from the human anaphylatoxin C5a receptor". The Journal of Biological Chemistry 270 (34): 19828–32. August 1995. doi:10.1074/jbc.270.34.19828. PMID 7649993. 
  • "Stabilization of C5a receptor--G-protein interactions through ligand binding". Journal of Cellular Biochemistry 55 (3): 380–8. July 1994. doi:10.1002/jcb.240550316. PMID 7962171. 
  • "Human chemotaxis receptor genes cluster at 19q13.3-13.4. Characterization of the human C5a receptor gene". Biochemistry 32 (5): 1243–50. February 1993. doi:10.1021/bi00056a007. PMID 8383526. 
  • "Molecular cloning and characterization of the human anaphylatoxin C3a receptor". The Journal of Biological Chemistry 271 (34): 20231–4. August 1996. doi:10.1074/jbc.271.34.20231. PMID 8702752. 
  • "CD88 antibodies specifically bind to C5aR on dermal CD117+ and CD14+ cells and react with a desmosomal antigen in human skin". Journal of Immunology 157 (4): 1729–35. August 1996. PMID 8759762. 
  • "The C5a chemoattractant receptor mediates mucosal defence to infection". Nature 383 (6595): 86–9. September 1996. doi:10.1038/383086a0. PMID 8779720. Bibcode: 1996Natur.383...86H. 
  • "Residues 21-30 within the extracellular N-terminal region of the C5a receptor represent a binding domain for the C5a anaphylatoxin". The Journal of Biological Chemistry 273 (17): 10411–9. April 1998. doi:10.1074/jbc.273.17.10411. PMID 9553099. 
  • "Expression of receptors for C5a anaphylatoxin (CD88) on human bronchial epithelial cells: enhancement of C5a-mediated release of IL-8 upon exposure to cigarette smoke". Journal of Immunology 160 (10): 5073–81. May 1998. PMID 9590258. 
  • "rC5a directs the in vitro migration of human memory and naive tonsillar B lymphocytes: implications for B cell trafficking in secondary lymphoid tissues". Journal of Immunology 162 (11): 6510–7. June 1999. PMID 10352266. 
  • "Stable expression of HIV-1 Nef induces changes in growth properties and activation state of human astrocytes". AIDS 13 (17): 2331–41. December 1999. doi:10.1097/00002030-199912030-00004. PMID 10597774. 
  • "Function, structure and therapeutic potential of complement C5a receptors". British Journal of Pharmacology 152 (4): 429–48. October 2007. doi:10.1038/sj.bjp.0707332. PMID 17603557. 

External links




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