Rescue of R137H mutant by SCTR as reflected by reduced affinity to β-arrestin.

Abstract

<p>The affinity between WT or mutant AVPR2 with β-arrestin were determined by BRET, using AVRP2 tagged with Rlu and β-arrestin tagged with YFP. A) In the native state, the R137H mutant shows significantly higher affinity to β-arrestin than the WT AVPR2. While the two other mutants, A89P and Q174R, showed slightly higher BRET than the WT receptor, but the increase was not significant. Upon co-expression of SCTR, β-arrestin affinity of R137H was significantly reduced compared to the scenario when no SCTR was present. B) BRET was measured at 10 min after addition of 1μM Vp to stimulate receptor internalization. WT AVPR2 showed increase affinity to β-arrestin, but not the R137H mutant without SCTR co-expression. With SCTR, R137H demonstrated increased β-arrestin binding, suggesting functional rescue of the receptor. Data are presented as means±SEM from three independent experiments in duplicate. ***, P<0.001, **, P<0.01.</p

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