|
|
|
|
|
| LOCAL
DEHYDROGENATION OF THE C11 HYDROXYL GROUP ON |
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| CORTISOL
PROTECTS MINERALOCORTICOID RECEPTORS (MR) |
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| FROM
INAPPROPRIATE ACTIVATION |
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|
|
|
| ALDOSTERONE:MR Kd~1nM |
||
| CORTISOL or CORTISONE : MR Kd~1nM |
||
| CORTISOL or
CORTISONE : GR Kd~10nM |
||
|
|
|
|
|
| IN
SPITE OF THE HIGH AFFINITY OF CORTISOL / CORTISONE FOR THE MR IN |
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| VITRO,
GLUCOCORTICOIDS DO NOT BIND TO MR IN TARGET TISSUES. THIS IS |
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| DUE TO THE
“PRE-RECEPTOR INACTIVATION” OF CORTISOL BY 11ß-HSD2 |
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| CORTISOL |
| CORTISOL |
| 11ß-HSD2 |
| 11ß-HSD1 |
| CORTISOL |
| CORTISONE |
| GR |
| MR |
| nucleus |
| nucleus |