Τόμος 24 (2010) – Τεύχος 2 – Άρθρο 63 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 24 (2010) – Issue 2 – Article 63 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title Regulator of G protein signaling 4: a novel regulator of μ– and δ-opioid receptor signaling
Authors Leonidas J. Leontiadis, Maria P. Papakonstantinou and Zafiroula Georgoussi

Laboratory of Cellular Signaling and Molecular Pharmacology, Institute of Biology, National Centre for Scientific Research Demokritos, Athens, Greece

Citation Leontiadis, L.J., Papakonstantinou, M.P., Georgousi, Z.: Regulator of G protein signaling 4: a novel regulator of μ– and δ-Opioid receptor signaling, Epitheorese Klin. Farmakol. Farmakokinet. 24(2): 168-170 (2010)
Publication Date 2010
Full Text Language English
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Keywords Regulator of G protein signaling, G protein, internalization, extracellular signal-regulated kinases, protein-protein interactions.
Other Terms Review article
Summary In vitro studies have shown that the Regulator of G protein Signaling 4 (RGS4) interacts with the C-termini of μ– and δ-opioid receptors (μ-OR, δ-OR) (1). Herein we demonstrate that RGS4 associates with these receptors in living cells and forms selective complexes with Gi/o proteins in a receptor dependent manner. This interaction occurs within the predicted fourth intracellular loop of μ, δ-ORs as part of a signaling complex consisting of the opioid receptor, activated Gα and RGS4. Expression of RGS4 in HEK293 cells attenuated agonist-mediated ERK1,2 phosphorylation for both receptors and accelerated agonist-induced internalization of the δ-OR. Our findings demonstrate that RGS4 plays a key role in G protein coupling selectivity and signaling of the μ– and δΟRs.
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