Recent advances in the study of 11 β-Hydroxysteroid dehydrogenase type 2(110-HSD2 inhibitors

摘要

11β-Hydroxysteroid dehydrogenase (l1β-HSD), which interconverts hormonally active Cortisol and inactive cortisone in multiple human tissues, has two distinct isoforms named 11 β-hydroxysteroid dehydrogenase 1 (11β-HSD1) and 11 β-hydroxysteroid dehydrogenase 2 (11β-HSD2). 11β-HSD2 is an NAD+-dependent oxidase which lowers Cortisol by converting it to cortisone while l1β-HSDl mainly catalyzes the reduction which converts cortisone into Cortisol. Selective inhibition of 11P-HSD2 is generally detrimental to health because the accumulation of Cortisol can cause metabolic symptoms such as apparent mineralocorticoid excess (AME), fetal developmental defects and lower testosterone levels in males. There has been some advances on the study of 11 β-HSD2 inhibitors and we think it necessary to make a summary of the characteristics and inhibiting properties of latest 11 β-HSD2 inhibitors. As another review on 11β-HSD2 inhibitors has been issued on 2011 (see review (Ma et al„ 2011)), this mini-review concerns advances during the last 5 years.