Biased signaling of the angiotensin II type 1 receptor can be mediated through distinct mechanisms.

ABSTRACT:

Background

Seven transmembrane receptors (7TMRs) can adopt different active conformations facilitating a selective activation of either G protein or β-arrestin-dependent signaling pathways. This represents an opportunity for development of novel therapeutics targeting selective biological effects of a given receptor. Several studies on pathway separation have been performed, many of these on the Angiotensin II type 1 receptor (AT1R). It has been shown that certain ligands or mutations facilitate internalization and/or recruitment of β-arrestins without activation of G proteins. However, the underlying molecular mechanisms remain largely unresolved. For instance, it is unclear whether such selective G protein-uncoupling is caused by a lack of ability to interact with G proteins or r

SUBMITTER: Bonde MM 

PROVIDER: S-EPMC2994726 | biostudies-literature | 2010 Nov

REPOSITORIES: biostudies-literature