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Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists.
- S. Stauffer, C. Coletta, J. Katzenellenbogen
- Biology, ChemistryJournal of medicinal chemistry
- 28 November 2000
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.
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
- M. J. Meyers, J. Sun, K. Carlson, G. Marriner, B. Katzenellenbogen, J. Katzenellenbogen
- Chemistry, BiologyJournal of medicinal chemistry
- 16 October 2001
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.
Nongenotropic, Sex-Nonspecific Signaling through the Estrogen or Androgen Receptors Dissociation from Transcriptional Activity
Phenol red in tissue culture media is a weak estrogen: implications concerning the study of estrogen-responsive cells in culture.
- Y. Berthois, J. Katzenellenbogen, B. Katzenellenbogen
- BiologyProceedings of the National Academy of Sciences…
- 1 April 1986
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.
Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression
The estradiol pharmacophore: Ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site
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…
Activating ESR1 Mutations Differentially Affect the Efficacy of ER Antagonists.
Although many mutations lead to constitutive activity and reduced sensitivity to ER antagonists, only select mutants such as Y537S caused a magnitude of change associated with fulvestrant resistance in vivo, which point to a need for antagonists with optimal pharmacokinetic properties to realize clinical efficacy against certain ESR1 mutants.
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
Propyl pyrazole triol (PPT) was found to be as efficacious as 17α-ethinyl-17β-estradiol in stimulating uterine weight gain and up-regulating complement 3 gene expression and was also effective in the brain.