Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships

Singh, Ranee, Reed, Anthony N., Chu, Peifei, Scully, Conor C. G., Yau, Mei-Kwan, Suen, Jacky Y., Durek, Thomas, Reid, Robert C. and Fairlie, David P. (2015) Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships. Bioorganic and Medicinal Chemistry Letters, 25 23: 5604-5608. doi:10.1016/j.bmcl.2015.10.038


Author Singh, Ranee
Reed, Anthony N.
Chu, Peifei
Scully, Conor C. G.
Yau, Mei-Kwan
Suen, Jacky Y.
Durek, Thomas
Reid, Robert C.
Fairlie, David P.
Title Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships
Journal name Bioorganic and Medicinal Chemistry Letters   Check publisher's open access policy
ISSN 1464-3405
0960-894X
Publication date 2015-12-01
Year available 2015
Sub-type Article (original research)
DOI 10.1016/j.bmcl.2015.10.038
Open Access Status Not Open Access
Volume 25
Issue 23
Start page 5604
End page 5608
Total pages 5
Place of publication Kidlington, Oxford United Kingdom
Publisher Pergamon Press
Collection year 2016
Language eng
Formatted abstract
Potent ligands for the human complement C3a receptor (C3aR) were developed from the almost inactive tripeptide Leu-Ala-Arg corresponding to the three C-terminal residues of the endogenous peptide agonist C3a. The analogous Leu-Ser-Arg was modified by condensing the serine side chain with the leucine carbonyl with elimination of water to form leucine-oxazole-arginine. Subsequent elaboration with a variety of N-terminal amide capping groups produced agonists as potent as human C3a itself in stimulating Ca2+ release from human macrophages. Structure–activity relationships are discussed.
Keyword C3aR agonist
C3a
Oxazole
Complement
Inflammation
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2016 Collection
Institute for Molecular Bioscience - Publications
 
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