The Regulator of G Protein Signaling Homologous Domain of G Protein-Coupled Receptor Kinase 2 Mediates Short-Term Desensitization of β3-Adrenergic Receptor
- Echeverría, Emiliana Beatriz
- Cabrera, Maia Diana Eliana
- Burghi, Valeria
- Sosa, Máximo Hernán
- Ripoll, Sonia
- Yaneff, Agustín
- Monczor, Federico
- Davio, Carlos Alberto
- Shayo, Carina Claudia
- Fernandez, Natalia Cristina
DOIAbstract
G protein coupled receptor (GPCR) kinases (GRKs) are key regulators of GPCR signaling. Canonical mechanism of GPCR desensitization involves receptor phosphorylation by GRKs followed by arrestin recruitment and uncoupling from heterotrimeric G protein. Although β3-adrenergic receptor (β3AR) lacks phosphorylation sites by GRKs, agonist treatment proved to induce β3AR desensitization in many cell types. Here we show that GRK2 mediates short-term desensitization of β3AR by a phosphorylation independent mechanism but mediated by its domain homologous to the regulator of G protein signaling (RGS). HEK293T cells overexpressing human β3AR presented a short-term desensitization of cAMP response stimulated by the β3AR agonist, BRL37344, and not by fo...
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