[HTML][HTML] Constitutive internalization of constitutively active angiotensin II AT1A receptor mutants is blocked by inverse agonists

S Miserey-Lenkei, C Parnot, S Bardin, P Corvol… - Journal of Biological …, 2002 - ASBMB
As constitutively active mutants (CAMs) mimic an active conformation, they can be used to
characterize the process of G protein-coupled receptor activation. Here, we used CAMs to
study the link between activation and internalization of the angiotensin II AT 1A receptor. The
cellular localization of fluorescently tagged N111A, I245T, and L305Q mutants was
determined by confocal microscopy. In the absence of ligand, CAMs were mostly located in
intracellular vesicles, whereas the wild-type AT 1A was found at the cell surface. After 2 h …