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 -