Endocrine Abstracts

The glucocorticoid receptor antagonist, RU486, binds to the glucocorticoid receptor (GR) with high affinity, and allows both nuclear localisation and also DNA binding. However, the DNA bound GR does not activate target gene transcription. This suggests that the ligand-binding domain of the GR is required to interpret agonist and antagonist ligands, and transmit those signals to the basal transcriptional machinery. Adaptor proteins play an important role in transducing the effe...

Glucocorticoids (Gc) are highly potent anti-inflammatory agents. They act through the glucocorticoid receptor (GR), a protein capable of multiple protein interactions. The pro-inflammatory cytokines, TNF-a and IL-1 signal, in part, through activation of NF-kB. Nf-kB transactivation is inhibited by activated GR. It has been suggested that the GR, and the p65 (RelA) component of NF-kB form a direct contact independent of Gc ligand, and that Gc binding results in inhibition of p6...

Glucocorticoids (Gcs) exert their pleiotropic effects through activation of the ubiquitously expressed glucocorticoid receptor (GR). The mechanism of transcriptional activation by the GR involves interaction with co-modulator proteins. Glucocorticoid sensitivity is mediated by the expression level of these co-modulator proteins and GR concentration. Therefore, the aim of this study was to identify additional GR interacting proteins that may influence glucocorticoid sensitivity...

(This poster is based on OC29)...

Glucocorticoids (Gc) act through the glucocorticoid receptor (GR) to regulate gene transcription, but also initiate a number of rapid non-genomic effects. The inactive GR is found complexed with hsp90 and immunophilins. Several other signalling molecules including c-src and raf-1 also associate with hsp90. Evidence suggests that Gc treatment results in the rapid activation and dissociation of GR and c-src from these complexes. We speculate that GR-mediated activation of one or...

Glucocorticoid sensitivity is dependent on the intracellular concentration of the glucocorticoid receptor (GR). GR expression is regulated in a complex, cell-type specific manner, but in most cell types the GR is subject to negative autoregulation by glucocorticoid exposure. Many human diseases are associated with reduced tissue sensitivity to glucocorticoids, including inflammatory arthritis, asthma, and chronic obstructive pulmonary disease. Therefore there is interest in ap...