Species dependence for binding of small molecule agonist and antagonists to the C5a receptor on polymorphonuclear leukocytes

Woodruff, Trent M., Strachan, Anna J., Sanderson, Sam D., Monk, Peter N., Wong, Allan K., Fairlie, David P. and Taylor, Stephen M. (2001) Species dependence for binding of small molecule agonist and antagonists to the C5a receptor on polymorphonuclear leukocytes. Inflammation, 25 3: 171-177. doi:10.1023/A:1011036414353


Author Woodruff, Trent M.
Strachan, Anna J.
Sanderson, Sam D.
Monk, Peter N.
Wong, Allan K.
Fairlie, David P.
Taylor, Stephen M.
Title Species dependence for binding of small molecule agonist and antagonists to the C5a receptor on polymorphonuclear leukocytes
Journal name Inflammation   Check publisher's open access policy
ISSN 0360-3997
1573-2576
Publication date 2001-06-01
Sub-type Article (original research)
DOI 10.1023/A:1011036414353
Volume 25
Issue 3
Start page 171
End page 177
Total pages 7
Editor B. N. Cronstein
Place of publication Plenum Press
Publisher New York
Language eng
Subject C1
06 Biological Sciences
Abstract This study investigated the receptor binding affinities of a C5a agonist and cyclic antagonists for polymorphonuclear leukocytes (PMNs) isolated from human, sheep, pig, dog, rabbit, guinea pig, rat and mouse. The affinities of the two small molecule antagonists, F-[OPdChaWR] and AcF-[OPdChaWR], and the agonist, YSFKPMPLaR, revealed large differences in C5a receptor (C5aR) affinities between species. The antagonists bound to human, rat and dog PMNs with similar high affinities, but with lower affinities to PMNs from all other species. The C5a agonist also bound with varying affinities between species, but showed a different affinity profile to the antagonists. In contrast, recombinant human C5a had similar affinity for PMNs of all species investigated. The low correlation between the affinities of the antagonists and the agonist between species either suggests that different receptor residues are important for distinguishing between agonist/antagonist binding, or that the agonist and antagonist peptides bind to two distinct sites within the C5aR.
Keyword Cell Biology
Immunology
C5a Antagonist
C5a Agonist
Leukocytes
Protein-coupled Receptors
Anaphylatoxin Receptor
Pharmacological Characterization
Cloning
Terminus
Analogs
Region
Rat
Activation
Expression
Q-Index Code C1

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Biomedical Sciences Publications
 
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Created: Wed, 15 Aug 2007, 02:46:35 EST