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Glucocorticoid receptor blockers

Pituitary, 2022
Mifepristone 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, 2007
Glucocorticoid 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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Glucocorticoid Receptors

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 and Bone

Current Pharmaceutical Design, 2010
Glucocorticoid 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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Regulation of glucocorticoid receptor gamma (GRγ) by glucocorticoid receptor haplotype and glucocorticoid

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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Glucocorticoid receptors

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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CORTICOSTEROIDS | Glucocorticoid Receptors

2006
Corticosteroids 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, 2008
This 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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