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Synthetic estrogens have diverse chemical structures and may either positively or negatively affect the estrogenic signaling pathways through interactions with the estrogen receptors (ERs). Modeling studies suggest that 4-(1-adamantyl)phenol (AdP) and 4,4'-(1,3-adamantanediyl)diphenol (AdDP) can bind in the ligand binding site of ERalpha. We used fluorescence polarization (FP) to compare the binding affinities of AdP, AdDP and 2-(1-adamantyl)-4-methylphenol (AdMP) for human ERalpha and ERbeta with the binding affinities of the known ER ligands, diethylstilbestrol (DES) and 4hydroxytamoxifen (4OHT). Competition binding experiments show that AdDP has greater affinity for both ERs than does AdP, while AdMP does not bind the receptor proteins. The relative binding affinities of AdDP and AdP are weaker than the affinity of DES or 4OHT for both ERs with the exception of AdDP, which binds ERbeta with higher affinity than does 4OHT. We also found that AdDP and AdP cause differential conformational changes in ERalpha and ERbeta, which result in altered affinities of the ERs for fluorescein-labeled estrogen response elements (EREs) using a direct binding FP assay. The results show that ERbeta liganded with either AdDP or AdP has greater affinity for human pS2 ERE than the ERbeta-4OHT complex. The data suggest that synthetic molecules like adamantanes may function as biologically active ligands for human ERs. This demonstrates the importance of considering the potential of novel classes of synthetic compounds as selective ER modulators.
INSERM, IFR105 Université Paris 7, INSERM, U553, Hémostase, Endothélium et Angiogénèse, Hôpital Saint Louis, 1 Avenue Claude Vellefaux, 75475 Paris Cedex 10, France
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INSERM, IFR105 Université Paris 7, INSERM, U553, Hémostase, Endothélium et Angiogénèse, Hôpital Saint Louis, 1 Avenue Claude Vellefaux, 75475 Paris Cedex 10, France
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INSERM, IFR105 Université Paris 7, INSERM, U553, Hémostase, Endothélium et Angiogénèse, Hôpital Saint Louis, 1 Avenue Claude Vellefaux, 75475 Paris Cedex 10, France
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INSERM, IFR105 Université Paris 7, INSERM, U553, Hémostase, Endothélium et Angiogénèse, Hôpital Saint Louis, 1 Avenue Claude Vellefaux, 75475 Paris Cedex 10, France
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compounds, polychlorinated biphenyls (PCBs), polychlorinated dibenzodioxins, organochlorine pesticides, and bisphenol A (BPA), have been shown or suspected to disrupt endocrine functions in animals. Generally, endocrine disruptors have estrogenic activity
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( Khaodhiar et al . 1999 ). The disease incidence is primarily related to a central, android fat distribution, typical for males ( Blaak 2001 ). Epidemiological and experimental studies link estrogen to the maintenance and distribution of body fat. This
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Estrogens are synonymous with fertility and infertility in mammals. Our knowledge of the biological actions of estrogens, however, is incomplete. Three recent developments have thrown new light on the actions of estrogens in mammalian reproduction that will lead to a greater understanding of their functions. They are (a) the identification of a second estrogen receptor, called ERbeta, (b) the identification of ligand-specific ER coactivators and (c) mouse models with targeted disruption of the genes encoding both ER and the aromatase enzyme. These models provide for the first time animals which are either unable to respond to endogenous or exogenous estrogens (ER 'knockouts'), or can respond to exogenous estrogen but do not make endogenous estrogen (aromatase 'knockout' or ArKO). Furthermore, the ArKO mouse has provided a model to study the effects on the ovary of exogenous estrogens of plant and synthetic origin that are of clinical relevance. The data show that estrogens are essential for fertility but not for survival after birth or for the formation of the reproductive tract. This commentary focuses on the roles of estrogen in folliculogenesis and in the maintenance of the ovarian somatic cell phenotype in the mouse. We also hypothesize that the ERalpha and ERbeta may subserve the proliferative and differentiative actions of estrogen, respectively, within a follicle. In summary, estrogen is obligatory for normal folliculogenesis beyond the antral stage and for the maintenance of the female phenotype of the somatic cells within the ovaries. This clearly demonstrates a major role for sex steroids in somatic cell differentiation in the gonads of eutherian mammals and challenges the central paradigm that the ovary is the default gonad, arising due to the absence of testicular defining signals. Evidence is also provided for the plasticity of the adult female gonad. Understanding the mechanisms of estrogen actions will provide an insight into the regulation of reproductive disorders afflicting women today, notably ovarian dysfunction and the menopause.
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Guangzhou Institute of Cardiovascular Disease, Guangzhou Key Laboratory of Cardiovascular Disease, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou, China
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Guangzhou Institute of Cardiovascular Disease, Guangzhou Key Laboratory of Cardiovascular Disease, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou, China
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Guangzhou Institute of Cardiovascular Disease, Guangzhou Key Laboratory of Cardiovascular Disease, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou, China
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studies have discovered that abnormal estrogen levels are associated with the occurrence of obesity, hypertension and coronary heart disease ( Taylor & Sullivan 2016 , Leeners et al. 2017 , Fortini et al. 2019 ). Epidemiological studies have shown
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secreting a substantial amount of estrogen. Furthermore, in our latest work, we clearly demonstrated that gastric estrogen but not gonadal estrogen directly stimulated ghrelin expression and production in the rat stomach ( Sakata et al . 2006
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treatment option because of its minimal side effects and relative ease of administration. Theoretically, ovarian cancer is a hormone-sensitive tumor. Previous studies have shown that the expression of estrogen receptors (ERα and ERβ) was detectable in 60
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Introduction Although 40–60% of ovarian cancers express estrogen receptor (ER) α ( Greenlee et al. 2000 , Havrilesky et al. 2001 ), only a minor proportion of patients (ranging from 7 to 18%) respond clinically to treatment with
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Department of Otorhinolaryngology, Center for Hearing and Communication Research, Department of Biosciences and Nutrition, Department of Woman and Child Health, Department of Biology and Biochemistry, Karolinska Institutet and Karolinska University Hospital, 171 76 Stockholm, Sweden
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. 1998 ). The hormone estradiol-17-β is thought to play an important role as estrogen receptors (ERs) are present in the inner ear at locations important for sound transmission ( Stenberg et al . 1999 ). Women at menopause with hormonal replacement
Department of spinal surgery, enji Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai, China
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. 2014 ). Puberty is the second growth peak in mammals. Endochondral ossification is regulated by multiple endocrine factors, especially during puberty ( Giustina et al. 2008 , Chagin & Sävendahl 2009 , Albrethsen et al. 2020 ). Estrogen is a key
