Structural Stereochemistry of Androstene Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoid Receptors
Year: 2013
Type: article
Abstract: DHEA, 17 α -AED, 17 β -AED, and 17 β -AET exhibit strong biological activity that has been attributed to androgenic, estrogenic, or antiglucocorticoid activity in vivo and in vitro. This study compared DHEA, 17 α -AED, 17 β -AED, and 17 β -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, ER α , and ER β 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.
DOI: 10.1155/2013/203606
Authors: Thomas L. Shaak, Dayanjan S. Wijesinghe, Charles E. Chalfant, Robert F. Diegelmann, Kevin R. Ward, Roger M. Loria
Language: English
Subfield: Genetics
Domain: Life Sciences
Open Access status: hybrid
Funders: U.S. Department of Defense, U.S. Department of Veterans Affairs, Virginia Commonwealth University, National Institutes of Health, U.S. Air Force, National Heart, Lung, and Blood Institute, National Cancer Institute, National Center for Research Resources, Medical Research and Materiel Command
Awards: The Role of Ceramide Kinase in Eicosanoid Synthesis, G2214260122, G4119534169, G4670433464, G4799061886, G5770983250, G5850682332, G5916161707, G6236649921, G6298840109, Regulation of caspase 9 RNA splicing in NSCLC cancer, G6822895880, CONSTRUCTION OF SIGNALLING FACILITY, G7483374307, G8173979607, G8316474997, G8371218060
OpenAlex ID: W2137935525