Impact of b2-adrenergic receptor polymorphisms in heart failure: Cell surface expression and internalization

Abstract

Heart Failure (HF) represents a major health problem throughout all over the world. One of the most cardiotoxic effects of HF is chronic catecholamine hypersecretion. In the heart, we can find β2-Adrenergic Receptors (β2-AR). β2-AR are known to be activated by catecholamines such as epinephrine and in consequence of this activation, receptors are internalized. It has been shown that certain polymorphisms of the β2-AR respond differently to ligand stimulation therefore being correlated with the severity of HF. These polymorphisms are: R16G, Q27E and T164I. We performed ELISA assays on HEK cells expressing β2-AR polymorphisms in order to determine β2-AR cell surface basal expression and internalization after epinephrine stimulation. We observed no differences with the WT on receptor cell surface expression and internalization for the β2-AR polymorphisms Q27E and T164I while polymorphism R16G showed an increased receptor cell surface expression and a decreased internalization post epinephrine stimulation.