Structural Stereochemistry of Androstene Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoid Receptors
Joint Authors
Ward, Kevin R.
Shaak, Thomas L.
Loria, Roger M.
Wijesinghe, Dayanjan S.
Chalfant, Charles E.
Diegelmann, Robert F.
Source
International Journal of Medicinal Chemistry
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-04-04
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
DHEA, 17α-AED, 17β-AED, and 17β-AET exhibit strong biological activity that has been attributed to androgenic, estrogenic, or antiglucocorticoid activity in vivo and in vitro.
This study compared DHEA, 17α-AED, 17β-AED, and 17β-AET for their ability to activate the human AR, ER, and GR and determine the relative androgenicity, estrogenicity, and glucocorticoid activity.
The results show that, at the receptor level, these androstene hormones are weak AR and even weaker ER activators.
Direct androstene hormone activation of the human AR, ERα, and ERβ may not be essential for their biological function.
Similarly, these hormones indirectly activated the human GR, only in the presence of high dexamethasone concentrations.
These results underscore the major difference between androstene hormone interactions with these nuclear receptors and their biological effects.
American Psychological Association (APA)
Shaak, Thomas L.& Wijesinghe, Dayanjan S.& Chalfant, Charles E.& Diegelmann, Robert F.& Ward, Kevin R.& Loria, Roger M.. 2013. Structural Stereochemistry of Androstene Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoid Receptors. International Journal of Medicinal Chemistry،Vol. 2013, no. 2013, pp.1-8.
https://search.emarefa.net/detail/BIM-454165
Modern Language Association (MLA)
Shaak, Thomas L.…[et al.]. Structural Stereochemistry of Androstene Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoid Receptors. International Journal of Medicinal Chemistry No. 2013 (2013), pp.1-8.
https://search.emarefa.net/detail/BIM-454165
American Medical Association (AMA)
Shaak, Thomas L.& Wijesinghe, Dayanjan S.& Chalfant, Charles E.& Diegelmann, Robert F.& Ward, Kevin R.& Loria, Roger M.. Structural Stereochemistry of Androstene Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoid Receptors. International Journal of Medicinal Chemistry. 2013. Vol. 2013, no. 2013, pp.1-8.
https://search.emarefa.net/detail/BIM-454165
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-454165