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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.
Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
TLDR
The messenger RNA expression of both ER subtypes in rat tissues by RT-PCR is investigated and the ligand binding specificity of the ER sub types is compared to contribute to the selective action of ER agonists and antagonists in different tissues.
Cloning of a novel receptor expressed in rat prostate and ovary.
TLDR
It is concluded that clone 29 cDNA encodes a novel rat ER, which is suggested be named rat ERbeta to distinguish it from the previously cloned ER (ERalpha) from rat uterus.
Mechanisms of estrogen action.
Our appreciation of the physiological functions of estrogens and the mechanisms through which estrogens bring about these functions has changed during the past decade. Just as transgenic mice were
Estrogen receptors: how do they signal and what are their targets.
TLDR
This review focuses on several of the interesting recent discoveries concerning estrogen receptors, on estrogen as a morphogen, and on the molecular mechanisms of anti-estrogen signaling.
Differential ligand activation of estrogen receptors ERalpha and ERbeta at AP1 sites.
TLDR
The transactivation properties of the two estrogen receptors, ERalpha and ERbeta, were examined with different ligands in the context of an estrogen response element and an AP1 element, suggesting that the two ERs may play different roles in gene regulation.
Generation and reproductive phenotypes of mice lacking estrogen receptor beta.
TLDR
The generation of mice lacking estrogen receptor beta (ERbeta -/-) is described by insertion of a neomycin resistance gene into exon 3 of the coding gene by using homologous recombination in embryonic stem cells to determine the role of ERbeta in bone and cardiovascular homeostasis.
Principles for modulation of the nuclear receptor superfamily
TLDR
This review provides a general overview of the mechanism of action of nuclear receptors and explores the various factors that are instrumental in modulating their pharmacology.
The different roles of ER subtypes in cancer biology and therapy
TLDR
The changes in the bioavailability of ERs in tumours promote the selective restoration of their activity as one of the major therapeutic approaches for hormone-dependent cancers.
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