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Glucocorticoid receptor blockers
Pituitary, 2022Mifepristone is the only glucocorticoid receptor antagonist currently approved for the treatment of Cushing's syndrome. Although originally developed as an abortifacient due to its blockade of the progesterone receptor, a number of case reports documented its efficacy as a glucocorticoid receptor blocker going back to 1985. The SEISMIC trial, published
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Glucocorticoid receptor physiology
Reviews in Endocrine and Metabolic Disorders, 2007Glucocorticoid action in cells is mediated by a specific receptor protein, the glucocorticoid receptor (GR). GR is a member of a superfamily of ligand-inducible transcription factors that control a variety of physiological functions; such as, metabolism, development, and reproduction.
Marjet D, Heitzer +4 more
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1979
Glucocorticoid receptors are found in most mammalian tissues and have been studied in detail in a number of tissue culture systems. With cells that have not been exposed to steroids, the receptors are found in the cytoplasmic fraction from which they can be isolated and studied.
G G, Rousseau, J D, Baxter
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Glucocorticoid receptors are found in most mammalian tissues and have been studied in detail in a number of tissue culture systems. With cells that have not been exposed to steroids, the receptors are found in the cytoplasmic fraction from which they can be isolated and studied.
G G, Rousseau, J D, Baxter
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Glucocorticoid Receptors and Bone
Current Pharmaceutical Design, 2010Glucocorticoid Receptors (GRs) have been identified in all bone cells. The molecular structure of human GR is organized into 3 major functional domains: the N-terminal immunogenic domain, the central DNA-binding domain and the C-terminal ligand-binding domain. Human GR is a product of a gene composed of 10 exons, located in the chromosome 5q31-32.
La Corte R, Trotta F, ADAMI, Silvano
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Clinical Endocrinology, 2004
Summaryobjective To measure glucocorticoid receptor gamma (GRγ) expression in transformed lymphocytes from individuals of known GR gene haplotype. Recently, a glucocorticoid receptor haplotype (GAT) has been described that associates with increased sensitivity to dexamethasone.
Stevens, Adam +2 more
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Summaryobjective To measure glucocorticoid receptor gamma (GRγ) expression in transformed lymphocytes from individuals of known GR gene haplotype. Recently, a glucocorticoid receptor haplotype (GAT) has been described that associates with increased sensitivity to dexamethasone.
Stevens, Adam +2 more
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The Journal of Steroid Biochemistry and Molecular Biology, 1992
Glucocorticoid hormones are secreted uniquely from the zona fasciculata of the adrenal cortex, with marked circadian variation in basal levels and acute elevation in response to stress. Glucocorticoid receptors are almost ubiquitously distributed, and mediate a wide range of tissue-specific responses; in addition to classical, [3H]dexamethasone-binding
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Glucocorticoid hormones are secreted uniquely from the zona fasciculata of the adrenal cortex, with marked circadian variation in basal levels and acute elevation in response to stress. Glucocorticoid receptors are almost ubiquitously distributed, and mediate a wide range of tissue-specific responses; in addition to classical, [3H]dexamethasone-binding
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CORTICOSTEROIDS | Glucocorticoid Receptors
2006Corticosteroids bind to and activate a cytoplasmic glucocorticoid receptor (GR) which exists as several isoforms derived from a single gene product by alternative splicing. The activated glucocorticoid receptor translocates into the nucleus and binds to specific response elements in the promoter regions of anti-inflammatory genes such as lipocortin-1 ...
Adcock I. M. +3 more
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Glucocorticoid Receptor Antagonists
Current Topics in Medicinal Chemistry, 2008This review covers recent progress in the discovery of selective glucocorticoid receptor (GR) antagonists. Potential therapeutic applications of selective GR antagonists are described including the pharmacological rationale and, in some cases, clinical evidence that underlies these proposed uses. Disease areas that are discussed are Cushing's syndrome,
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