Chapter 31 - Glucocorticoid compounds in drug discovery by targeting glucocorticoid receptor protein

Abstract

Glucocorticoids targeting the glucocorticoid receptor (GR) as the most potent and effective agents for treating inflammation disease are widely used on the drug market. However, even at therapeutic dosages, these glucocorticoids induce a series of undesired side effects. Owing to these undesirable side effects and given the widespread prevalence of inflammation in the world, the discovery and development of a new generation of antiinflammatory drug by targeting GRs, which retain their beneficial therapeutic effects but reduce adverse side effects, is urgent. Here, we concisely introduce the developments of glucocorticoids and discuss the action of mechanism of the GR-mediated signaling pathway. Based on this, some representative marketed glucocorticoid drugs and our main contributions by targeting GRs are summarized. Finally, an outlook is given on how to develop a new generation of glucocorticoid-based drugs with powerful antiinflammatory activity and lower side effects.