11β-Hydroxysteroid Dehydrogenases (11β-HSD) isozymes 11β-HSD1 and 11β-HSD2 catalyze the interconversion of cortisol and cortisone. 11β-HSD1 converts cortisone to cortisol, the active hormone; and 11β-HSD2 converts cortisol to cortisone, the inactive form.
Inhibitors |
Cat. No. | Product Name / Activity |
---|---|
3096 | Carbenoxolone disodium |
Inhibitor of 11β-hydroxysteroid dehydrogenase. Also gap junction blocker | |
3291 | PF 915275 |
Potent and selective 11β-hydroxysteroid dehydrogenase inhibitor |
The isozymes 11β-HSD1 and 11β-HSD2, both 11β-Hydroxysteroid Dehydrogenases (11β-HSD), catalyze the interconversion of cortisol (corticosterone in rodents) and cortisone (11-dehyrodocorticosterone). 11β-HSD1 converts cortisone to cortisol, the active hormone; and 11β-HSD2 converts cortisol to cortisone, the inactive form.
Cortisol is initially synthesized and released by the adrenal glands under the strict control of adrenocorticotrophic hormone (ACTH). Levels vary in response to physical and psychological stress. As the name suggests, glucocorticoids increase and maintain blood glucose levels; cortisol also increases blood pressure, inhibits bone growth and contributes to cognitive dysfunction. Due to their integral role in glucocorticoid homeostasis, 11β-HSD1 and 11β-HSD2 may be important factors in the development of conditions such as hypertension, depression, osteoporosis, type 2 diabetes, and obesity.
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Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
---|---|---|---|---|
11-HSD1 | Human | HSD11B1 | NM_005525 | P28845 |
Mouse | Hsd11b1 | NM_008288 | P50172 | |
Rat | Hsd11b1 | NM_017080 | Q6TUH9 | |
11-HSD2 | Human | HSD11B2 | NM_000196 | U14631 |
Mouse | Hsd11b2 | NM_008289 | P51661 | |
Rat | Hsd11b2 | NM_017081 | P50233 |