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Vol. 61, Issue 3, 546-553, March 2002
Centre Hospitalier Universitaire de Québec, Centre de
Recherche du Pavillon l'Hôtel-Dieu de Québec,
Québec, Canada
The kallikrein-kinin system, activated during inflammatory conditions
and the regulation of specific cardiovascular and renal functions,
includes two G protein-coupled receptors for bradykinin (BK)-related
peptides. The B1 receptor (B1R) subtype is not
believed to undergo agonist-induced phosphorylation and endocytosis. A conjugate made of the rabbit B1R fused with the yellow
variant of green fluorescent protein (YFP) was expressed in mammalian cells. In COS-1 or human embryonic kidney (HEK) 293 cells, the construction exhibited a nanomolar affinity for the agonist radioligand [3H]Lys-des-Arg9-BK or the antagonist ligand
[3H]Lys-[Leu8]des-Arg9-BK and a
pharmacological profile virtually identical to that of wild-type
B1R. Lys-des-Arg9-BK stimulation of HEK 293 cells stably expressing B1R-YFP but not stimulation of
untransfected cells released [3H]arachidonate in a
phospholipase A2 assay. B1R-YFP was visualized as a continuous labeling of the plasma membranes in stably transfected HEK 293 cells (confocal microscopy). Addition of
Lys-des-Arg9-BK (1-100 nM) rapidly concentrated the
receptor-associated fluorescence into multiple aggregates that remained
associated with the plasma membrane (no significant internalization)
and colocalized with caveolin-1. This reaction was slowly reversible
upon agonist washing at 37°C and prevented pretreatment with a
B1R antagonist. 
-Cyclodextrin treatment, which extracts
cholesterol from membranes and disrupts caveolae-related rafts,
prevented agonist-induced redistribution of B1R-YFP but not
the PLA2 activation mediated by this receptor. The agonist
radioligand copurified with caveolin-1 to a greater extent than the
tritiated antagonist in buoyant fractions of HEK 293 cells treated with
the ligands. Agonist-induced cellular translocation of the kinin
B1R to caveolae-related rafts without endocytosis is a
novel variation on the theme of G protein-coupled receptor adaptation.
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