The inhibition of human and rat 11β-hydroxysteroid dehydrogenase 2 by perfluoroalkylated substances
Zhao, B; Lian, Q; Chu, Y; Hardy, DO; Li, XK; Ge, RS
HERO ID
1402568
Reference Type
Journal Article
Year
2011
Language
English
PMID
| HERO ID | 1402568 |
|---|---|
| In Press | No |
| Year | 2011 |
| Title | The inhibition of human and rat 11β-hydroxysteroid dehydrogenase 2 by perfluoroalkylated substances |
| Authors | Zhao, B; Lian, Q; Chu, Y; Hardy, DO; Li, XK; Ge, RS |
| Journal | Journal of Steroid Biochemistry and Molecular Biology |
| Volume | 125 |
| Issue | 1-2 |
| Page Numbers | 143-147 |
| Abstract | 11β-Hydroxysteroid dehydrogenase 2 (11β-HSD2) regulates active glucocorticoid access to glucocorticoid and mineralocorticoid receptors by metabolizing it to an inactive form. Perfluoroalkylated substances (PFASs) are man-made polyfluorinated compounds that are widely used and persistent in the environment. We tested the inhibitory potencies of four PFASs including perfluorooctanoic acid (PFOA), perfluorooctane sulfonate (PFOS), perfluorohexanesulfonate (PFHxS) and perfluorobutane sulfonate (PFBS) on human and rat 11β-HSD2. PFOS was a potent inhibitor of both human (IC(50)=48 nM) and rat (IC(50)=293 nM) 11β-HSD2 activities. The potencies for the inhibition of human and rat 11β-HSD2 activities were PFOS>PFOA>PFHxS>PFBS. PFASs showed competitive inhibition of both human and rat 11β-HSD2 activities. This observation indicates that PFOS is a potent endocrine disruptor for glucocorticoid metabolism. Article from the Special issue on Targeted Inhibitors. |
| Doi | 10.1016/j.jsbmb.2010.12.017 |
| Pmid | 21237268 |
| Wosid | WOS:000292174400016 |
| Is Certified Translation | No |
| Dupe Override | No |
| Comments | Source: Web of Science WOS:000292174400016Scopus URL: https://www.scopus.com/inward/record.uri?eid=2-s2.0-79957770534&doi=10.1016%2fj.jsbmb.2010.12.017&partnerID=40&md5=9f67d7c51a81f0b786326b880a7989e4 |
| Is Public | Yes |
| Language Text | English |
| Keyword | 11 beta-Hydroxysteroid dehydrogenase 2; Human kidney; Perfluorinated substances; Perfluoroalkyl acids; Perfluorooctyl sulphonate; Perfluorohexyl sulfonate; Perfluorobutyl sulphonate; Perfluorooctanoic acid |