Τόμος 20 (2006) – Τεύχος 2 – Άρθρο 69 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 20 (2006) – Issue 2 – Article 69 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title Signal transduction differences between  WT and polymorphic α2Β-adrenergic receptor in LLC-PK1 Cells
Authors Orthodoxia Mastrogianni¹, George Karkoulias¹, Herve Paris² and Christodoulos Flordellis¹

1. Department of Pharmacology, School of Medicine, University of Patras, 26110 Rio Patras, Greece

2. INSERM U388, Institut Louis Bugnard, CHU Rangueil, Toulouse, France

Citation Mastrogianni, Ο., Karkoulias, Γ., Paris, Η., Flordellis, Ch: Signal transduction differences between  WT and polymorphic α2Β-adrenergic receptor in LLC-PK1 Cells, Epitheorese Klin. Farmakol. Farmakokinet. 20(2): 249-250 (2006)
Publication Date Accepted for publication: 19-20 May 2006
Full Text Language English
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Keywords α2Β-adrenergic receptor, MAPK, Akt, NF-κB, IKKα/β.
Other Terms review article
Summary The aim of the present study was to characterise the signaling pathway triggered by activated human α2B-adrenergic receptor in trasfected LLC-PK1, a renal tubular cell line. Moreover to investigate differences between the wild-type (WT) and a polymorphic α2B-AR (MUT), which has a deletion of three glutamic acids (Del301-303) in its third intracellular loop. Upon agonist stimulation with UK 14304, both receptors (WT and MUT) induced ERK1/2 phosphorylation, whilst this phosphorylation was abolished by prior treatment of the cells with LY 240092, a pharmacological inhibitor of PI3K. Treatment of the cells with UK 14304 induced IKK phosphorylation and NF-KB-driven luciferase activity and this activation was abolished by prior treatment of the cells with LY 240092. The activation of IKK/NF-κB from the polymorphic adrenoceptor was absolutely dependent on prior ERK activation, in clear demarcation to WT-induced NF-κB activation, which is ERK independent.
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