C5a receptor

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C5AR1
Identifiers
AliasesC5AR1, C5A, C5AR, C5R1, CD88, complement component 5a receptor 1, C5a receptor, complement C5a receptor 1
External IDsOMIM: 113995 MGI: 88232 HomoloGene: 20413 GeneCards: C5AR1
Gene location (Human)
Chromosome 19 (human)
Chr.Chromosome 19 (human)[1]
Chromosome 19 (human)
Genomic location for C5AR1
Genomic location for C5AR1
Band19q13.32Start47,290,023 bp[1]
End47,322,066 bp[1]
RNA expression pattern
PBB GE C5AR1 220088 at fs.png
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001736

NM_001173550
NM_007577

RefSeq (protein)

NP_001727

NP_001167021
NP_031603

Location (UCSC)Chr 19: 47.29 – 47.32 MbChr 7: 16.25 – 16.26 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

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.[5] C5a receptor modulates inflammatory responses, obesity, development and cancers.[6][7][8]

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

Cells[edit]

The C5a receptor is expressed on:[9]

Agonist and antagonists[edit]

Potent and selective agonist and antagonists for C5aR have been developed.[10][11][12][13]

See also[edit]

References[edit]

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000197405 - Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000049130 - 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. ^ Gerard C, Gerard NP (1994). "C5A anaphylatoxin and its seven transmembrane-segment receptor". Annual Review of Immunology. 12: 775–808. doi:10.1146/annurev.iy.12.040194.004015. PMID 8011297.
  6. ^ Brennan FH, Gordon R, Lao HW, Biggins PJ, Taylor SM, Franklin RJ, Woodruff TM, Ruitenberg MJ (April 2015). "The Complement Receptor C5aR Controls Acute Inflammation and Astrogliosis following Spinal Cord Injury". The Journal of Neuroscience. 35 (16): 6517–31. doi:10.1523/JNEUROSCI.5218-14.2015. PMC 6605214. PMID 25904802.
  7. ^ 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.
  8. ^ Markiewski MM, DeAngelis RA, Benencia F, Ricklin-Lichtsteiner SK, Koutoulaki A, Gerard C, Coukos G, Lambris JD (November 2008). "Modulation of the antitumor immune response by complement". Nature Immunology. 9 (11): 1225–35. doi:10.1038/ni.1655. PMC 2678913. PMID 18820683.
  9. ^ 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.
  10. ^ Wong AK, Finch AM, Pierens GK, Craik DJ, Taylor SM, Fairlie DP (August 1998). "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. doi:10.1021/jm9800651. PMID 9719594.
  11. ^ Gong Y, Barbay JK, Buntinx M, Li J, Wauwe JV, Claes C, Lommen GV, Hornby PJ, He W (July 2008). "Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 18 (14): 3852–5. doi:10.1016/j.bmcl.2008.06.059. PMID 18595693.
  12. ^ Sumichika H, Sakata K, Sato N, Takeshita S, Ishibuchi S, Nakamura M, Kamahori T, Ehara S, Itoh K, Ohtsuka T, Ohbora T, Mishina T, Komatsu H, Naka Y (December 2002). "Identification of a potent and orally active non-peptide C5a receptor antagonist". The Journal of Biological Chemistry. 277 (51): 49403–7. doi:10.1074/jbc.M209672200. PMID 12384495.
  13. ^ Seow V, Lim J, Cotterell AJ, Yau MK, Xu W, Lohman RJ, Kok WM, Stoermer MJ, Sweet MJ, Reid RC, Suen JY, Fairlie DP (April 2016). "Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists". Scientific Reports. 6 (1): 24575. doi:10.1038/srep24575. PMC 4837355. PMID 27094554.

Further reading[edit]

External links[edit]