Regulation of membrane cholecystokinin-2 receptor by agonists enables classification of partial agonists as biased agonists.

ABSTRACT: Given the importance of G-protein-coupled receptors as pharmacological targets in medicine, efforts directed at understanding the molecular mechanism by which pharmacological compounds regulate their presence at the cell surface is of paramount importance. In this context, using confocal microscopy and bioluminescence resonance energy transfer, we have investigated internalization and intracellular trafficking of the cholecystokinin-2 receptor (CCK2R) in response to both natural and synthetic ligands with different pharmacological features. We found that CCK and gastrin, which are full agonists on CCK2R-induced inositol phosphate production, rapidly and abundantly stimulate internalization. Internalized CCK2R did not rapidly recycle to plasma membrane but instead was directed to late endos

SUBMITTER: Magnan R 

PROVIDER: S-EPMC3057855 | biostudies-literature | 2011 Feb

REPOSITORIES: biostudies-literature