Ligand-Mediated Regulation of Kinin Receptors in the Rabbit
François Marceau, Albert Adam, Steeve Houle, Johanne Bouthillier, Magdalena Bachvarova, Dimcho Bachvarov
Abstract
François Marceau, Albert Adam, Steeve Houle, Johanne Bouthillier, Magdalena Bachvarova, Dimcho Bachvarov
Abstract
The kinin B1 receptors (B1Rs), stimulated by des-Arg9-kinins, are completely inducible, notably following treatment of animals with bacterial lipopolysaccharide. Several studies based on cultured cells have suggested a form of autoregulation of kinin receptors, because B2 receptor (B2R) or B1R stimulation could transcriptionally upregulate B1R expression. The B2R may rather be downregulated in inflammatory conditions. A rabbit B2R-green fluorescent protein (GFP) conjugate stably expressed in HEK 293 cells was rapidly internalized in response to the agonist bradykinin. Ligand-induced receptor cycling was documented applying confocal microscopy. The results confirm agonist-induced B2R endocytosis, but extensive recycling to the cell membrane does not support agonist-induced downregulation.
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The kinin B1 receptors (B1Rs), stimulated by des-Arg9-kinins, are completely inducible, notably following treatment of animals with bacterial lipopolysaccharide. Several studies based on cultured cells have suggested a form of autoregulation of kinin receptors, because B2 receptor (B2R) or B1R stimulation could transcriptionally upregulate B1R expression. The B2R may rather be downregulated in inflammatory conditions. A rabbit B2R-green fluorescent protein (GFP) conjugate stably expressed in HEK 293 cells was rapidly internalized in response to the agonist bradykinin. Ligand-induced receptor cycling was documented applying confocal microscopy. The results confirm agonist-induced B2R endocytosis, but extensive recycling to the cell membrane does not support agonist-induced downregulation.
Key concepts: Kinin, Receptor, Agonist, Bradykinin, Downregulation and upregulation, Cell biology, Chemistry, Bradykinin receptor