Estrogens cross-talk to alpha1b-adrenergic receptors

Molecular Pharmacology
Aliesha González-ArenasJ A García-Sáinz

Abstract

beta-Estradiol induced alpha1b-adrenergic receptor desensitization in U373 MG cells stably expressing alpha1b-adrenoceptors, as evidenced by a reduction in the adrenergic-mediated Ca2+ mobilization; desensitization was associated with receptor phosphorylation and internalization. These effects of beta-estradiol were rapid (taking place during 15 min) and were blocked by the estrogen receptor antagonist ICI 182,780 (faslodex). Likewise, inhibitors of phosphoinositide 3-kinase [wortmannin and 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002)] and of protein kinase C [staurosporine, 3-[1-[3-(amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl) maleimide (Ro31-8220), and rottlerin] blocked the desensitization and phosphorylation of alpha1b-adrenoceptors induced by estradiol. The formation of a complex was suggested by coimmunoprecipitation assays. The regulatory and catalytic subunits of phosphoinositide 3-kinase (p85 and p110) and protein kinase C delta were associated with alpha1b-adrenoceptors in the absence of stimulus, and such association further increased in a dynamic fashion in response to beta-estradiol. In cells cotransfected with the estrogen receptor alpha and alpha1b-adrenoceptors, beta-estradiol indu...Continue Reading

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Citations

Apr 16, 2010·Canadian Journal of Physiology and Pharmacology·Natalia Ziolkowski, Ashok K Grover
Mar 24, 2009·Autonomic & Autacoid Pharmacology·R Alcántara-Hernández, J Adolfo García-Sáinz
Oct 22, 2010·Endocrine·Olivia Tania Hernández-HernándezIgnacio Camacho-Arroyo
Aug 5, 2011·IUBMB Life·J Adolfo García-SáinzRocío Alcántara-Hernández
Oct 5, 2007·European Journal of Pharmacology·Tzindilú Molina-MuñozJ Adolfo García-Sáinz
Aug 28, 2021·International Journal of Molecular Sciences·Paola MatarreseGiuseppe Marano
Jan 2, 2008·Biochimica Et Biophysica Acta·Aliesha González-ArenasJ Adolfo García-Sáinz
Jan 5, 2011·Archives of Medical Research·Juan José MandokiFausto Alejandro Jiménez-Orozco
Oct 25, 2011·Biochimica Et Biophysica Acta·Jean A Castillo-BadilloJ Adolfo García-Sáinz

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