Τόμος 22 (2008) – Τεύχος 2 – Άρθρο 59 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 22 (2008) – Issue 2 – Article 59 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title RGS4 and RGS2 differentially modulate opioid receptor signaling
Authors L.J. Leontiadis, M.-P. Papakonstantinou, M. Sarris snd Z. Georgoussi

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

Citation Leontiadis, L.J., Papakonstantinou, M.-P., Sarris, M., Georgousi, Z.: RGS4 and RGS2 differentially modulate opioid receptor signaling, Epitheorese Klin. Farmakol. Farmakokinet. 22(2): 214-216 (2008)
Publication Date 23-25 May 2008
Full Text Language English
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Keywords GPCRs, opioid receptors, RGS4, RGS2, receptor internalization.
Other Terms Review article
Summary Regulators of G protein signaling (RGS) comprise a large family of proteins possessing intrinsic GAP (GTPase activating protein) activity that manifest their action upon members of the G proteins to modulate the signaling of G protein coupled receptors (GPCRs). Recent observations reveal that these proteins can serve as effector antagonists, as scaffolds recruiting novel interacting partners and can directly interact with GPCRs to modulate their signaling events. In order to elucidate the role of RGS proteins in opioid receptor signaling pathways we focused on two members of the B/R4 subfamily, namely RGS4 and RGS2 proteins. In this respect, we were able to demonstrate for the first time that a) localization of RGS4 and RGS2 can be affected by μ– and δ– opioid receptor activation and b) the rate of the internalization of opioid receptors is differentially regulated by RGS4 and RGS2.
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2. Georgoussi Z.: Novel Interacting Partners Regulating Opioid Receptor Signaling. In: Molecular Aspects of G Protein-Coupled Receptors (Ciruela F. and Lujan R., eds). Chapter 6: 169-205, Nova Science Publishers, Inc., 2008

3. Georgoussi Z., Merkouris M., Mullaney I., Megaritis G., Carr C., Zioudrou C. and Milligan C.: Selective interactions of μ-opioid receptors with Pertussis toxin-sensitive G proteins: involvement of the third intracellular loop and the C-terminal tail in coupling. Biochim. Biophys. Acta 1359: 263-274 (1997)

4. Mazarakou G., Georgoussi Z.: STAT5A interacts with and is phosphorylated upon activation of the mu-opioid receptor. J. Neurochem. 93: 918-931 (2005)

5. Morou E., Gergoussi Z.: Expression of the third intracellular loop of the delta-opioid receptor inhibits signaling by opioid receptors and other G protein-coupled receptors. J. Pharmacol. Exp. Ther. 315: 1368-1379 (2005)

6. Georgoussi Z., Leontiadis L., Mazarakou G., Merkouris M., Hyde K. and Hamm H.: Selective interactions between G protein subunits and RGS4 with the C-terminal domains of the mu- and delta-opioid receptors regulate opioid receptor signaling. Cell Signal 18: 771-782 (2006)

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