糖皮质激素受体拮抗剂的作用机制研究与相关药物开发

Researches on the Mechanism of Action of Glucocorticoid Receptor Antagonists and the Related Drug Development

综述糖皮质激素受体介导的糖异生机制以及该受体激动剂和拮抗剂的作用机制,分类介绍糖皮质激素受体拮抗剂的研究与开发。早期的糖皮质激素受体拮抗剂米非司酮具有较好的活性,但同时具有抗孕激素作用,选择性差,副作用多,因此,寻找和发现高选择性的糖皮质激素受体拮抗剂已成为抗2型糖尿病药物研究的新领域。

The mechanism of glucocorticoid receptor（GR）-mediated gluconeogensis and GR agonism and antagonism was reviewed. The research and development of GR antagonists were introduced classifiedly. Early GR antagonist mifepristone shows good activity, but at the same time it has anti-progestogen activity, poorspecificity and more side effects. So screening and finding of high specific GR antagonists have become a new field of research on anti-type 2 diabetes drugs.