What are the physiological estrogens?

@article{Baker2013WhatAT,
  title={What are the physiological estrogens?},
  author={Michael E. Baker},
  journal={Steroids},
  year={2013},
  volume={78},
  pages={337-340}
}
  • M. Baker
  • Published 1 March 2013
  • Medicine, Chemistry
  • Steroids
View on Elsevier
doi.org
41 Citations
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41 Citations

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The promiscuous estrogen receptor: Evolution of physiological estrogens and response to phytochemicals and endocrine disruptors
  • M. Baker, R. Lathe
  • Medicine, Biology
    The Journal of Steroid Biochemistry and Molecular Biology
  • 2018
The promiscuous estrogen receptor: evolution of physiological estrogens and response to phytochemicals and endocrine disruptors
TLDR
Structural diversity in the A ring of physiological estrogens can explain the response of the ER to synthetic chemicals, which disrupt estrogen physiology in vertebrates, and the estrogenic activity of a variety of plant-derived chemicals such as genistein, coumestrol, and resveratrol.
Estrogen Physiology from an Evolutionary Perspective
TLDR
Dobzhansky's insight that “Nothing in Biology Makes Sense Except in the Light of Evolution” is adapted to estrogen physiology to provide an evolutionary perspective for these novel estrogens and their physiological actions in the brain and other organs.
Expanding the structural footprint of xenoestrogens
Many synthetic chemicals with structural similarity to estradiol bind to the estrogen receptor and disrupt the normal estrogen physiology in humans and other vertebrates. Most of these xenoestrogens…
MECHANISMS IN ENDOCRINOLOGY: Estradiol as a male hormone.
TLDR
The collective evidence suggests that, in men, E2 is an important hormone for hypothalamic-pituitary-testicular axis regulation, reproductive function, growth hormone-insulin-like growth factor-1 axisregulation, bone growth and maintenance of skeletal health, body composition and glucose metabolism, and vasomotor stability.
Origin of the response to adrenal and sex steroids: Roles of promiscuity and co-evolution of enzymes and steroid receptors
Biological effects induced by estrogenic activity of lignans
Evolution of Steroid Receptors
Steroid signaling: Ligand-binding promiscuity, molecular symmetry, and the need for gating
TLDR
Counter-intuitively, the specificity of steroid/sterol action is achieved not by intrinsic binding selectivity but by the combination of local metabolism and binding affinity.
The Role of Estrogen in Brain and Cognitive Aging
TLDR
E2 treatment has been shown to ameliorate some of the behavioral and morphological changes seen in preclinical models of menopause; however, in clinical populations, the effects of E2 treatment on cognitive changes after menopausal transition are mixed.
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References

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Insights from the structure of estrogen receptor into the evolution of estrogens: implications for endocrine disruption.
  • M. Baker
  • Biology, Medicine
    Biochemical pharmacology
  • 2011
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TLDR
It is demonstrated here that 27-hydroxycholesterol (27HC), the most prevalent oxysterol in circulation, functions as a SERM, the efficacy of which varies when assessed on different endpoints, and it appears that the unique pharmacological activity of 27HC relates to its ability to impact ER structure and modulate cofactor recruitment.
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TLDR
It is demonstrated that the estrogen receptor (ER) α mediates gene expression changes and growth responses induced by 25HC in breast and ovarian cancer cells, and the estrogen-like activity of 25HC elicited in the cardiovascular system may play a role against hypoxic environments.
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TLDR
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TLDR
ADIOL is effective as an estrogen in MCF7 cells at a concentration of 2 nm, which is within the range found in the blood of normal women; sulfurylation is a major route of inactivation of 3β-hydroxy Δ5-steroids in MCf7 cells.
Binding characteristics of 5-androstene-3β, 17β-diol and estradiol-17β to the cytoplasmic estrogen receptor of the immature rat uterus
27-Hydroxycholesterol is an endogenous SERM that inhibits the cardiovascular effects of estrogen
TLDR
Increase in 27HC levels in mice by diet-induced hypercholesterolemia, pharmacologic administration or genetic manipulation decreased estrogen-dependent expression of vascular nitric oxide synthase and repressed carotid artery reendothelialization, indicating that 27HC functions as an endogenous selective estrogen receptor modulator (SERM).
Estrogen receptor β and 17β-hydroxysteroid dehydrogenase type 6, a growth regulatory pathway that is lost in prostate cancer
TLDR
Observations reveal that formation of 3β-Adiol via 17βHSD6 from DHT is an important growth regulatory pathway that is lost in prostate cancer.
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.
The endogenous selective estrogen receptor modulator 27-hydroxycholesterol is a negative regulator of bone homeostasis.
TLDR
It is found that increasing concentrations of 27HC led to decreased bone mineral density that was associated with decreased bone formation and increased bone resorption, and this data provides evidence for interactions between estrogen signaling, cholesterol and metabolic disease, and osteoporosis.
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