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

Abstract

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 telmi-sartan, 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.