Internalization of Constitutively Active N111G Mutant of AT1 Receptor Induced by Angiotensin II–Receptor Antagonists Candesartan, Losartan, and Telmisartan: Comparison With Valsartan

Internalization of Constitutively Active N111G Mutant of AT1 Receptor Induced by Angiotensin II–Receptor Antagonists Candesartan, Losartan, and Telmisartan: Comparison With Valsartan

Based on radioligand binding and signal transduction assays in our previous study, we have determined the binding pattern and functional efficacy of the constitutively active mutant N111G of angiotensin II type 1 (AT1) receptor. We have also shown that the N111G mutant induces homologous internaliza...

Full description

Bibliographic Details
Main Authors: Mohiuddin Ahmed Bhuiyan, Murad Hossain, Takashi Nakamura, Masanobu Ozaki, Takafumi Nagatomo
Format: Article
Language:English
Published: Elsevier 2010-01-01
Series:Journal of Pharmacological Sciences
Online Access:http://www.sciencedirect.com/science/article/pii/S134786131930982X
Description
Summary:Based on radioligand binding and signal transduction assays in our previous study, we have determined the binding pattern and functional efficacy of the constitutively active mutant N111G of angiotensin II type 1 (AT1) receptor. We have also shown that the N111G mutant induces homologous internalization through mediation of the AT1-receptor antagonist valsartan. In this study we demonstrated that other AT1-receptor antagonists, candesartan, losartan, and telmisartan, also stimulate internalization of N111G mutant receptor to the same extent. We further showed that the internalization pattern is also similar for all the AT1-receptor antagonists. Keywords:: angiotensin II type 1 (AT1) receptor, constitutively active mutant, internalization
ISSN:1347-8613

Similar Items