PMID: 11312148Apr 20, 2001Paper

The steroid receptor antagonists RU40555 and RU486 activate glucocorticoid receptor translocation and are not excreted by the steroid hormones transporter in L929 cells

The Journal of Endocrinology
C M ParianteA H Miller

Abstract

RU40555 is a recently available glucocorticoid receptor (GR) antagonist that differs from RU486 by a methyl radical. We have used the mouse fibroblast cell line L929 to study the in vitro effects of RU40555 on GR translocation and function and on the membrane steroid hormones transporter. The results showed that: 1) RU40555 competed for the binding of labelled dexamethasone (Dex) with a K(i) of 2.4 nM; 2) both RU40555 and RU486 were equally potent inhibitors of Dex-induced GR-mediated gene transcription; 3) maximum GR translocation induced by micromolar concentrations of Dex and the GR antagonists was approximately 30-55% loss in the cytoplasmic GR and approximately 40-90% increase in the nuclear GR (assessed by GR immunostaining in cytoplasm and nucleus and western blots of immunoprecipitated GR protein in cytosolic and nuclear fractions) and was similar for the two antagonists; 4) at nanomolar concentrations, RU40555 and RU486 induced more GR translocation than Dex (assessed by [(3)H]Dex binding and western blot of immunoreactive GR in the same cytosolic homogenates); 5) blocking the steroids membrane transporter with verapamil (100 microM) in the presence of Dex (10 nM) increased GR translocation to levels similar to those i...Continue Reading

Citations

Nov 8, 2003·Molecular and Cellular Endocrinology·Maria-M KoufaliKieran C Breen
Jan 30, 2004·Psychoneuroendocrinology·Carmine M ParianteRobert W Kerwin
May 23, 2002·Biological Psychiatry·Carmine M ParianteStafford Lightman
Aug 2, 2003·Molecular and Cellular Endocrinology·Beum-Soo AnEui-Bae Jeung
Mar 28, 2008·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Livia A CarvalhoCarmine M Pariante
Oct 14, 2004·European Journal of Biochemistry·Joanna E ChiversRobert Newton
Dec 10, 2008·Stress : the International Journal on the Biology of Stress·Livia A Carvalho, Carmine M Pariante
Apr 18, 2002·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·G G GibsonW El-Sankary
Feb 26, 2008·European Journal of Pharmacology·Renato Malcher-LopesJeffrey G Tasker
Oct 31, 2006·The Journal of Steroid Biochemistry and Molecular Biology·Sara SaponaroFrancesca Silvagno
Jul 23, 2003·British Journal of Pharmacology·Carmine M ParianteRobert W Kerwin
Sep 29, 2011·Traffic·Sofie VandevyverClaude Libert
Jul 15, 2004·Toxicology in Vitro : an International Journal Published in Association with BIBRA·A F MazonS E Wendelaar Bonga
Dec 1, 2003·Acta Neuropsychiatrica·Mario F JuruenaCarmine M Pariante
Aug 27, 2005·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Rachel YehudaLisa Tischler
Nov 7, 2003·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Richard C SheltonFridolin Sulser
Mar 8, 2014·Arteriosclerosis, Thrombosis, and Vascular Biology·Ling GuoXiang-An Li
Jun 5, 2003·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Carmine M ParianteRobert W Kerwin
Feb 24, 2006·Journal of Neuroscience Research·Yeasmin TaheraBarbara Canlon
Nov 9, 2007·Journal of Biomolecular Screening·Michele AglerTaosheng Chen
Jan 13, 2005·Revista brasileira de psiquiatria : orgão oficial da Associação Brasileira de Psiquiatria, Asociación Psiquiátrica de la América Latina·Mario F JuruenaCarmine M Pariante
May 6, 2021·International Journal of Molecular Sciences·Jeahee RyuYoungeun Kwon

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