糖皮质激素受体及其选择性调节剂研究进展

Research progresses in glucocorticoid receptor and selective glucocorticoid receptor modulators

糖皮质激素(glucocorticoids,GCs)是临床上广泛使用的一类抗炎药物,在体内主要通过糖皮质激素受体(glucocorticoid receptor,GR)发挥生理和药理作用。GR是核受体超家族的成员之一,为配体激活的转录因子,在机体的多种生理和病理活动中扮演重要的角色。随着对GR信号通路的深入研究,寻找针对糖皮质激素受体的新型调节剂,以期将抗炎作用和现有糖皮质激素的副作用相分离,已经成为新药发现的研究热点。本文对近年来GR的分子结构、生物学作用及其选择性调节剂的研究进展作一简要的介绍。

Glucocorticoids （GCs） are widely used as anti-inflammatory therapeutics. Their physiological and pharmacological actions are mainly mediated by glucocorticoid receptor （GR）. As a member of the nuclear receptor superfamily, GR is a ligand-activated transcriptional factor and plays important roles in many physiological and pathological processes. With in-depth knowledge on the molecular mechanisms involved in GR- related signal transduction pathways, discovery of novel GR modulators has become one of the focal points in drug development, aiming at increasing efficacies and reducing side effects. In this review, we briefly describe the current understanding of molecular structure, biological functions and selective modulators of GR.