International Union of Pharmacology. LXIV. Estrogen Receptors

@article{DahlmanWright2006InternationalUO,
  title={International Union of Pharmacology. LXIV. Estrogen Receptors},
  author={Karin Dahlman-Wright and Vincent Cavaill{\`e}s and Suzanne A. W. Fuqua and V Craig Jordan and John A. Katzenellenbogen and Kenneth S. Korach and Adriana Maggi and M. Muramatsu and M. G. Parker and Jan-{\AA}ke Gustafsson},
  journal={Pharmacological Reviews},
  year={2006},
  volume={58},
  pages={773 - 781}
}
Estrogen receptors (ERs[1][1]) are ligand-activated transcription factors that belong to the nuclear hormone receptor superfamily. In the late 1950s, the existence of a receptor molecule that could bind 17β-estradiol was demonstrated by Jensen and Jacobsen ([Jensen and Jordan, 2003][2]). The first 
ESR2 (Estrogen Receptor 2 (ER beta))
Review on ESR2 (Estrogen Receptor 2 (ER beta) ), with data on DNA, on the protein encoded, and where the gene is implicated.
Differential interactions of antiretroviral agents with LXR, ER and GR nuclear receptors: potential contributing factors to adverse events
TLDR
The closely related liver X receptors, oestrogen receptors and glucocorticoid receptor regulate many endogenous processes such as lipid/cholesterol homeostasis, cellular differentiation and inflammation.
The estrogen receptor: two or more molecules, multiple variants, diverse localizations, signaling and functions. Are we undergoing a paradigm-shift as regards their significance in breast cancer?
TLDR
This paper aims to demonstrate the efforts towards in-situ applicability of the EMT technique in the field of medicine and its applications in the context of regenerative medicine.
The unfolding stories of GPR30, a new membrane-bound estrogen receptor.
TLDR
The G protein-coupled and seven-transmembrane receptor, GPR30, is now widely recognized as an estrogen receptor (ER), hence its official new acronym GPER, and appears to mediate a wide range of responses to estrogen in a large variety of cell types.
27-Hydroxycholesterol, an endogenous selective estrogen receptor modulator.
The Estrogen Receptors: An Overview from Different Perspectives.
  • K. Eyster
  • Biology, Medicine
    Methods in molecular biology
  • 2016
TLDR
The purpose of this discussion of the estrogen receptors is to provide a brief overview of the hormone receptors and estrogen action from perspectives such as the historical, physiological, pharmacological, pathological, structural, and ligand perspectives.
International Union of Basic and Clinical Pharmacology. XCVII. G Protein–Coupled Estrogen Receptor and Its Pharmacologic Modulators
TLDR
The history and characterization of GPER over the past 15 years is described, focusing on the pharmacology of steroidal and nonsteroidal compounds that have been employed to unravel the biology of this most recently recognized estrogen receptor.
Nuclear Hormone Receptor Medicinal Chemistry
This chapter will be focused on recent advances in the medicinal chemistry of agonist, antagonist, and modulator ligands of selected nuclear hormone receptors (NHRs) that are of special interest in
...
...

References

SHOWING 1-10 OF 115 REFERENCES
Update on estrogen signaling
Identification of pathway-selective estrogen receptor ligands that inhibit NF-kappaB transcriptional activity.
TLDR
This pathway-selective ligand does not promote the classic actions of estrogens such as stimulation of uterine proliferation or ER-mediated gene expression, but is a potent antiinflammatory agent, as demonstrated in the HLA-B27 transgenic rat model of inflammatory bowel disease.
Identification of a splice variant of the rat estrogen receptor β gene
Molecular Determinants for the Tissue Specificity of SERMs
TLDR
It is shown that both tamoxifen and raloxifene induce the recruitment of corepressors to target gene promoters in mammary cells, which determines the cellular response to selective estrogen receptor modulators.
Identification of a splice variant of the rat estrogen receptor beta gene.
TLDR
A second, larger transcript appears to arise through differential splicing of the ligand-binding domain of the rat ERbeta cDNA, which has 54 nucleotides inserted after position 1372 encoding 18 additional amino acids.
Molecular basis of agonism and antagonism in the oestrogen receptor
TLDR
The crystal structures of the LBD of ER in complex with the endogenous oestrogen, 17β-oestradiol, and the selective antagonist raloxifene provide a molecular basis for the distinctive pharmacophore of the ER and its catholic binding properties.
Coregulators in nuclear estrogen receptor action: from concept to therapeutic targeting.
TLDR
This review describes current efforts aimed at developing pharmaceutical agents that target ER-cofactor interactions as therapeutics for estrogen-associated pathologies and provides an additional level of complexity in ER action.
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.
Estrogen Receptor α Mediates Estrogen’s Immune Protection in Autoimmune Disease
TLDR
Findings are central to the design of selective ER modifiers which aim to target biologic responses in specific organ systems.
...
...