A ligand-specific kinetic switch regulates glucocorticoid receptor trafficking and function
نویسندگان
چکیده
منابع مشابه
A ligand-specific kinetic switch regulates glucocorticoid receptor trafficking and function.
The ubiquitously expressed glucocorticoid receptor (GR) is a major drug target for inflammatory disease, but issues of specificity and target tissue sensitivity remain. We now identify high potency, non-steroidal GR ligands, GSK47867A and GSK47869A, which induce a novel conformation of the GR ligand-binding domain (LBD) and augment the efficacy of cellular action. Despite their high potency, GS...
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Word count 6912 (excluding references) 1 2 A ligand-specific kinetic switch regulates glucocorticoid receptor 3 trafficking and function. 4 5 Peter J Trebble 1,2 , James M Woolven 3 , Ken A Saunders 3 , Karen D Simpson 3 , Stuart N 6 Farrow 1,3 , Laura C Matthews 1,2 *, David W Ray 1,2 * 7 8 9 Running title: Ligand-specific regulation of GR action 10 11 1 Manchester Centre for Nuclear Hormone R...
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Robert J.G. Haché, Joanne G.A. Savory and Yvonne A. Lefebvre Departments of Medicine, Biochemistry, Microbiology and Immunology, The Loeb Health Research Institute at the Ottawa Hospital, University of Ottawa, 725 Parkdale Ave., Ottawa, Ontario, Canada, K1Y 4K9 ______________________________________________________________________________________________________ 3 Correspondence: Robert J.G. Ha...
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The glucocorticoid receptor (GR) is a member of the nuclear hormone receptor superfamily of ligand-activated transcription factors. In contrast to many other nuclear receptors, GR is thought to be exclusively cytoplasmic in quiescent cells, and only translocate to the nucleus on ligand binding. We now demonstrate significant nuclear GR in the absence of ligand, which requires nuclear localisati...
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ژورنال
عنوان ژورنال: Journal of Cell Science
سال: 2013
ISSN: 1477-9137,0021-9533
DOI: 10.1242/jcs.124784