Article
Inverse agonist activity of selected ligands of platelet-activating factor receptor.
The Journal of pharmacology and experimental therapeutics - 1 Oct 2001
Dupré D J, Le Gouill C, Rola-Pleszczynski M, Stanková J
Abstract excerpt
The receptor for platelet-activating factor (PAFR) is a member of the G protein-coupled receptor (GPCR) family. According to the allosteric ternary complex model, GPCRs exist in an equilibrium between different conformations. Agonist binding promotes and stabilizes the receptor in an active conformation. On the other hand, ligands that stabilize the inactive conformation are known as inverse agonists. Due to the...
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