RGS DOMAIN OF GRK2 MEDIATES β3-ADRENERGIC RECEPTOR DESENSITIZATION

FERNANDEZ, NATALIA; GRANJA GALEANO, GINA; SHAYO, CARINA; ECHEVERRIA, EMILIANA; MONCZOR, FEDERICO; CABRERA, MAIA

Buenos Aires

Congreso; REUNIÓN CONJUNTA DE SOCIEDADES DE BIOCIENCIAS; 2017

β3-adrenergic receptor (β3AR) belongs to the superfamily of G protein-coupled receptors and when activated mediates intracellular cAMP increase. It is mainly expressed in adipose tissues and bladder and has been postulated as target for the treatment of overactive bladder syndrome (OBS). Previous work in endogenously expressing β3AR SK-N-MC cells, showed that pre-treatment with isoproterenol led to a significant desensitization of the receptor. However, β3AR lacks potential sites for PKA or GRKs mediated phosphorylation, which have been previously demonstrated to be involved in β1AR and β2AR desensitization. The aim of the present work was to evaluate the mechanism of β3AR desensitization using HEK293T transfected cells.