TY - JOUR
A2 - Bednarski, Patrick
AU - Shaak, Thomas L.
AU - Wijesinghe, Dayanjan S.
AU - Chalfant, Charles E.
AU - Diegelmann, Robert F.
AU - Ward, Kevin R.
AU - Loria, Roger M.
PY - 2013
DA - 2013/04/04
TI - Structural Stereochemistry of Androstene Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoid Receptors
SP - 203606
VL - 2013
AB - 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.
SN - 2090-2069
UR - https://doi.org/10.1155/2013/203606
DO - 10.1155/2013/203606
JF - International Journal of Medicinal Chemistry
PB - Hindawi Publishing Corporation
KW -
ER -