Pyrazolo[1,5-a]pyrimidines: Estrogen Receptor Ligands Possessing Estrogen Receptor β Antagonist Activity.
نویسندگان
چکیده
منابع مشابه
Estrogen Receptor Activity
Natural estrogens modulate the activity of target cells by binding at least two intranuclear receptors. ERα and ERβ belong to a large family of structurally related transcription factors that are well conserved from the evolutionary and functional points of view. The considerable progress made recently in comprehending ER structure (figs. 6–1 and 6–2) and mechanism of action (fig. 6–2) provides...
متن کاملStructure-activity relationship model for estrogen receptor ligands
STRUCTURE-ACTIVITY RELATIONSHIP MODEL FOR ESTROGEN RECEPTOR LIGANDS Huihui Wu November 29,2011 Xenoestrogens are spread throughout the environment affecting our daily lives and may produce potential toxic effects on human health. The purpose of this study was to develop a mechanistically reliable model capable of identifying xenoestrogens. Our hypothesis was that there are identifiable structur...
متن کاملNovel Ligands that Function as Selective Estrogens or Antiestrogens for Estrogen Receptor-α or Estrogen Receptor-β.
We report on the identification of novel, nonsteroidal ligands that show pronounced subtype-selective differences in ligand binding and transcriptional potency or efficacy for the two estrogen receptor (ER) subtypes, ER alpha and ER beta. An aryl-substituted pyrazole is an ER alpha potency-selective agonist, showing higher binding affinity for ER alpha and 120-fold higher potency in stimulation...
متن کاملEstrogen Receptor Ligands: A Review (2013–2015)
Estrogen receptors (ERs) are a group of compounds named for their importance in both menstrual and estrous reproductive cycles. They are involved in the regulation of various processes ranging from tissue growth maintenance to reproduction. Their action is mediated through ER nuclear receptors. Two subtypes of the estrogen receptor, ERα and ERβ, exist and exhibit distinct cellular and tissue di...
متن کاملEstrogen-related receptor β (ERRβ) – renaissance receptor or receptor renaissance?
Estrogen-related receptors (ERRs) are founding members of the orphan nuclear receptor (ONR) subgroup of the nuclear receptor superfamily. Twenty-seven years of study have yet to identify cognate ligands for the ERRs, though they have firmly placed ERRα and ERRγ at the intersection of cellular metabolism and oncogenesis. The pace of discovery for novel functions of ERRβ, however, has until recen...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2005
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm058162z