Improving the Utility of Steroidal Anti-Inflammatories: Identification of Selective Glucocorticoid Receptor Modulators

Steroidal compounds such as prednisone and dexamethasone are full agonists of the glucocorticoid receptor (GR). They are enormously valuable in the treatment of a wide variety of inflammatory diseases. However, the value of these glucocorticoids is greatly limited by their side effects. Our increasing understanding of the molecular mechanisms involved in the activation of GR has provided new opportunities to discover and develop novel compounds that maintain the efficacy of currently used steroids but avoid some of the dose limiting side effects.