Novel ligands: fine tuning the transcriptional activity of the glucocorticoid receptor

Current Pharmaceutical Design
M Schulz, M Eggert

Abstract

Glucocorticoids are the first line medication used in the therapy of many severe inflammatory disorders. They exert their activity through binding to the glucocorticoid receptor, a ligand-dependent transcription factor, and result in either activation or repression of a large set of glucocorticoid responsive genes. The desired immunosuppressive effect is apparently due largely to the down-regulation of a variety of pro-inflammatory factors, whereas adverse reactions such as corticoid-induced diabetes and osteoporosis could be connected to the inappropriate activation of genes involved in the control of metabolic processes. The discovery of improved glucocorticoids, which maintain beneficial therapeutic activity together with a diminished risk of side effects, focuses on ligands that lead to repression rather than activation of genes targeted by the glucocorticoid receptor. Current drug-screening programs have yielded a number of molecules including steroidal as well as non-steroidal compounds, which preferentially induce receptor-mediated repression. The characterization of these novel glucocorticoids in several in vitro and in vivo models for their immune modulating activity marks an important step towards the development of a...Continue Reading

Citations

Apr 2, 2010·Oxidative Medicine and Cellular Longevity·Adel R A Abd-AllahSaleh A Al-Bakheet
Jul 17, 2007·Molecular and Cellular Endocrinology·Heike SchäckeKhusru Asadullah
Jun 2, 2007·Veterinary Immunology and Immunopathology·Johan BuyseBruno M Goddeeris
Apr 6, 2005·Bioorganic & Medicinal Chemistry Letters·Christopher F ThompsonSilvi Luell

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