Features of the shuttle pair 11 beta-hydroxyprogesterone-11-ketoprogesterone
Autor: | Mario D. Galigniana, Gerardo Burton, Guillermo P. Vicent, C.P. Lantos |
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Rok vydání: | 1997 |
Předmět: |
Male
Stereochemistry Clinical Biochemistry Dehydrogenase Biochemistry Binding Competitive Hop (networking) Rats Sprague-Dawley Endocrinology Mineralocorticoid receptor Glucocorticoid receptor Tyrosine aminotransferase Receptors Glucocorticoid Transcortin Chaps Hydroxyprogesterones Animals Molecular Biology Progesterone Tyrosine Transaminase Pharmacology biology Chemistry Organic Chemistry Sodium Hydroxysteroid Dehydrogenases Adrenalectomy Cholic Acids Hydrogen-Ion Concentration Rats Receptors Mineralocorticoid Enzyme Induction biology.protein Hydroxyprogesterone 11-beta-Hydroxysteroid Dehydrogenases |
Zdroj: | Steroids. 62(4) |
ISSN: | 0039-128X |
Popis: | 11β-hydroxyprogesterone (HOP) and 11-ketoprogesterone (KP) are reversible components of a shuttle pair whose interconversion in rat liver is catalyzed by isoform-1 of 11β-hydroxysteroid dehydrogenase. Kidneys also produce this interconversion. The present study was carried out to investigate the shuttle pair and its components in the rat. As in corticosterone/11-dehydrocorticosterone, oxidation is more effective at an alkaline pH, while reduction prevails at a neutral pH. Moreover, both reactions are inhibited by the detergent 3-[(3-cholamido propyl)-dimethylammonio]-1-propane-sulphonate (CHAPS). However, at variance with the 11-ketosteroids cortisone (E) and 11-dehydrocorticosterone (A) thought to be “inactive,” KP has slight direct Na + -retaining properties, and it, as well as HOP, induces glucocorticoids (11β-hydroxycorticoids) to retain sodium. 11-ketoprogesterone exhibits 17 times better affinity for native type I mineralocorticoid receptor than HOP and a 3-fold affinity for partially purified (transcortin free) mineralocorticoid receptor. However, KP, in contrast to HOP, binds only weakly to transcortin, not at all to glucocorticoid receptor, and requires reduction at C 11 for tyrosine aminotransferase (TAT) induction. |
Databáze: | OpenAIRE |
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