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Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists.
TLDR
Investigations suggest that the pyrazole triols prefer to bind to ERalpha with their C(3)-phenol in the estradiol A-ring binding pocket and that binding selectivity results from differences in the interaction of thePyrazole core and C(4)-propyl group with portions of the receptor where ERalpha has a smaller residue than ERbeta. Expand
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
TLDR
This study suggests that, in this series of ligands, the nitrile functionality is critical to ERbeta selectivity because it provides the optimal combination of linear geometry and polarity. Expand
Nongenotropic, Sex-Nonspecific Signaling through the Estrogen or Androgen Receptors Dissociation from Transcriptional Activity
TLDR
A novel paradigm of sex steroid action on osteoblasts, osteocytes, embryonic fibroblasts, and HeLa cells involving activation of a Src/Shc/ERK signaling pathway and attenuating apoptosis is demonstrated, providing proof of principle for the development of function-specific-as opposed to tissue-selective-and gender-neutral pharmacotherapeutics. Expand
Phenol red in tissue culture media is a weak estrogen: implications concerning the study of estrogen-responsive cells in culture.
TLDR
It is found that phenol red, which bears a structural resemblance to some nonsteroidal estrogens and which is used ubiquitously as a pH indicator in tissue culture media, has significant estrogenic activity at the concentrations (15-45 microM) at which it is found in tissueculture media. Expand
Equol, a natural estrogenic metabolite from soy isoflavones: convenient preparation and resolution of R- and S-equols and their differing binding and biological activity through estrogen receptors
TLDR
An efficient and convenient method to prepare (+/-)-equol from available isoflavanoid precursors is developed and the activities of the enantiomers on the two estrogen receptors, ERalpha and ERbeta are studied for the first time. Expand
Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression
TLDR
Because these ligands maintain their agonist or antagonist character and ER subtype-selectivity at gene sites of diverse nature, where estradiol is either stimulatory or inhibitory, these compounds should prove useful in elucidating the biological functions of ERalpha and ERbeta. Expand
The estradiol pharmacophore: Ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site
TLDR
The various elements in this model for the binding of steroidal estrogens by the estrogen receptor are consistent with evidence emerging from the crystal structures of related nuclear hormone receptor ligand complexes. Expand
Characterization of the Biological Roles of the Estrogen Receptors, ERα and ERβ, in Estrogen Target Tissues in Vivo through the Use of an ERα-Selective Ligand
Estrogens elicit many biomedically important responses in different target tissues, and the respective roles of the two estrogen receptors, ERα and ERβ, in mediating these bioactivities isExpand
Estrogen-occupied Estrogen Receptor Represses Cyclin G2 Gene Expression and Recruits a Repressor Complex at the Cyclin G2 Promoter*
TLDR
It is shown that cyclin G2 is a primary ER target gene in MCF-7 breast cancer cells that is rapidly and robustly down-regulated by estrogen and indicates a role for nuclear receptor corepressors and associated histone deacetylase activity in mediating negative gene regulation by this hormone-occupied nuclear receptor. Expand
An ADIOL-ERβ-CtBP Transrepression Pathway Negatively Regulates Microglia-Mediated Inflammation
TLDR
Evidence is provided that 5-androsten-3β,17β-diol (ADIOL) functions as a selective modulator of estrogen receptor (ER)β to suppress inflammatory responses of microglia and astrocytes and can be targeted by selective ERβ modulators. Expand
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