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Environ Toxicol Pharmacol. 2017 Jun;52:47-53. doi: 10.1016/j.etap.2017.02.021. Epub 2017 Mar 21.

Recent advances in the study of 11β-Hydroxysteroid dehydrogenase type 2 (11β-HSD2)Inhibitors.

Author information

1
The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 32500, China. Electronic address: zcc2899@163.com.
2
The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 32500, China.
3
The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 32500, China.
4
Wenzhou Central Hopital, Wenzhou, Zhejiang 32500, China.

Abstract

11β-Hydroxysteroid dehydrogenase (11β-HSD), which interconverts hormonally active cortisol and inactive cortisone in multiple human tissues, has two distinct isoforms named 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) and 11β-hydroxysteroid dehydrogenase 2 (11β-HSD2). 11β-HSD2 is an NAD+-dependent oxidase which lowers cortisol by converting it to cortisone while 11β-HSD1 mainly catalyzes the reduction which converts cortisone into cortisol. Selective inhibition of 11β-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 11β-HSD2 inhibitors and we think it necessary to make a summary of the characteristics and inhibiting properties of latest 11β-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.

KEYWORDS:

11β-Hydroxysteroid dehydrogenase type 2; Cortisol; Inhibitor; Metabolic symptoms

PMID:
28366868
DOI:
10.1016/j.etap.2017.02.021
[Indexed for MEDLINE]

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