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• W2068817981 abstract "Glucocorticosteroids are highly effective in the control of many inflammatory and immune diseases, and recently there has been an enormous increase in our understanding of the molecular mechanisms involved? Recently important advances have occurred in understanding the molecular mechanisms of steroid action, largely through the application of molecular biology techniques. 2, 3 GLUCOCORTICOID RECEPTORS Glucocorticoids exert their effects by binding to a single glucocorticoid receptor (GR), which is predominantly localized to the cytoplasm of target cells, and only on binding of the glucocorticoid does it move into the nuclear compartment. The affinity of cortisol binding to GR is approximately 30 mmol/L, which falls within the normal range for plasma concentrations of free hormone. There is a single class of GRs, with no evidence of subtypes of differing affinity in different tissues, and its structure has been elucidated with the use of sitedirected mutagenesis, which has revealed distinct domains. 4 The glucocorticoid-binding domain is at the C-terminal end of the molecule, and two finger-like projections that interact with DNA are in the middle of the molecule. Each of these fingers is formed by a zinc molecule bound to four cysteine residues. An N-terminal domain (-q) is involved in transcriptional trans-activation of genes once binding to DNA occurs, and this region may also be involved in binding to other transcription factors. 5 This is the least conserved part of the molecule. Deletion analysis has demonstrated a 41-amino acid core at the C-terminal end of the r a domain that is critical for trans-activation. In human GRs there is another trans-acting domain ('r2) adjacent to the steroid-binding domain, and this region is also important for the nuclear transloca" @default.
• W2068817981 created "2016-06-24" @default.
• W2068817981 creator A5030258071 @default.
• W2068817981 date "1996-01-01" @default.
• W2068817981 modified "2023-09-25" @default.
• W2068817981 title "Molecular mechanisms of steroid action in asthma" @default.
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• W2068817981 doi "https://doi.org/10.1016/s0091-6749(96)80216-8" @default.
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