Anaphylatoxin receptor promiscuity for commonly used complement C5a peptide agonists.
C3aR
C5aR1
C5aR1 agonists
C5aR2
Selectivity
Signalling
Journal
International immunopharmacology
ISSN: 1878-1705
Titre abrégé: Int Immunopharmacol
Pays: Netherlands
ID NLM: 100965259
Informations de publication
Date de publication:
Nov 2021
Nov 2021
Historique:
received:
11
06
2021
revised:
30
07
2021
accepted:
11
08
2021
pubmed:
29
8
2021
medline:
8
2
2022
entrez:
28
8
2021
Statut:
ppublish
Résumé
The complement system is an essential component of innate immunity. Its activation generates the effector cleavage proteins, anaphylatoxins C3a and C5a, that exert activity by interacting with three structurally related seven-transmembrane receptors. C3a activates C3aR, whilst C5a interacts with both C5aR1 and C5aR2 with equal potency. Of the three receptors, C5aR1 in particular is considered the most functionally potent inflammatory driver and has been the major target for pharmacological development. Multiple peptidic C5a agonists have been developed to target C5aR1, with the full agonists EP54 (YSFKPMPLaR) and EP67 (YSFKDMP(MeL)aR), and the partial agonist C028 (C5a
Identifiants
pubmed: 34454293
pii: S1567-5769(21)00710-4
doi: 10.1016/j.intimp.2021.108074
pii:
doi:
Substances chimiques
C5AR1 protein, human
0
C5aR2 protein, human
0
Oligopeptides
0
Peptide Fragments
0
Receptor, Anaphylatoxin C5a
0
Receptors, Complement
0
complement C3a receptor
0
complement C5a, (65-74), Tyr(65)-Phe(67)-Pro(69,71)-Ala(73)-
0
tyrosyl-seryl-phenylalanyl-lysyl-aspartyl-methionyl-prolyl-N-methyleucyl-alanyl-arginine
0
Complement C5a
80295-54-1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
108074Informations de copyright
Copyright © 2021 Elsevier B.V. All rights reserved.