scholarly journals The Role of Estriol and Estrone in Keratoconic Stromal Sex Hormone Receptors

2022 ◽  
Vol 23 (2) ◽  
pp. 916
Author(s):  
Paulina Escandon ◽  
Sarah E. Nicholas ◽  
Rebecca L. Cunningham ◽  
David A. Murphy ◽  
Kamran M. Riaz ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Stromal Cells ◽  
Estrogen Receptor Alpha ◽  
Hormone Receptors ◽  
Estrogen Receptor Beta ◽  
Corneal Stroma ◽  
Sex Hormone ◽  
Human Cornea

Keratoconus (KC) is a progressive corneal thinning disease that manifests in puberty and worsens during pregnancy. KC onset and progression are attributed to diverse factors that include: environmental, genetics, and hormonal imbalances; however, the pathobiology remains elusive. This study aims to determine the role of corneal stroma sex hormone receptors in KC and their interplay with estrone (E1) and estriol (E3) using our established 3D in vitro model. Healthy cornea stromal cells (HCFs) and KC cornea stromal cells (HKCs), both male and female, were stimulated with various concentrations of E1 and E3. Significant changes were observed between cell types, as well as between males and females in the sex hormone receptors tested; androgen receptor (AR), progesterone receptor (PR), estrogen receptor alpha (ERα), and estrogen receptor beta (ERβ) using Western blot analysis. E1 and E3 stimulations in HCF females showed AR, PR, and ERβ were significantly upregulated compared to HCF males. In contrast, ERα and ERβ had significantly higher expression in HKC’s females than HKC’s males. Our data suggest that the human cornea is a sex-dependent, hormone-responsive tissue that is significantly influenced by E1 and E3. Therefore, it is plausible that E1, E3, and sex hormone receptors are involved in the KC pathobiology, warranting further investigation.

scholarly journals ERα-Targeting PROTAC as a Chemical Knockdown Tool to Investigate the Estrogen Receptor Function in Rat Menopausal Arthritis

2021 ◽  
Vol 12 ◽  
Author(s):  
Li Duan ◽  
Xiao Xu ◽  
Limei Xu ◽  
Caining Wen ◽  
Kan Ouyang ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Alpha ◽  
Gene Knockouts ◽  
Matrix Metabolism ◽  
Or Gene ◽  
Genetic Compensation ◽  
Embryonic Death

Proteolytic targeting chimeras (PROTACs) is a rapid and reversible chemical knockout method. Compared with traditional gene-editing tools, it can avoid potential genetic compensation, misunderstandings caused by spontaneous mutations, or gene knockouts that lead to embryonic death. To study the role of estrogen receptor alpha (ERα) in the occurrence and progression of menopausal arthritis, we report a chemical knockout strategy in which stable peptide-based (PROTACs) against ERα to inhibit their function. This chemical knockdown strategy can effectively and quickly inhibit ERα protein in vivo and in vitro. In the rat menopausal arthritis model, this study showed that inhibiting estrogen function by degrading ERα can significantly interfere with cartilage matrix metabolism and cause menopausal arthritis by up-regulating matrix metalloproteinase (MMP-13). The results of this study indicate that ERα is a crucial estrogen receptor for maintaining cartilage metabolism. Inhibition of ERα function by PROTACs can promote the progression of osteoarthritis.

scholarly journals Estrogen receptor beta in prostate cancer: friend or foe?

2014 ◽  
Vol 21 (4) ◽  
pp. T219-T234 ◽  
Author(s):  
Adam W Nelson ◽  
Wayne D Tilley ◽  
David E Neal ◽  
Jason S Carroll
Keyword(s):  
Prostate Cancer ◽  
Estrogen Receptor ◽  
Animal Studies ◽  
Estrogen Receptor Alpha ◽  
Estrogen Receptor Beta ◽  
Cancer Cell Line ◽  
Future Research ◽  
Prostate Carcinogenesis ◽  
Receptor Beta

Prostate cancer is the commonest, non-cutaneous cancer in men. At present, there is no cure for the advanced, castration-resistant form of the disease. Estrogen has been shown to be important in prostate carcinogenesis, with evidence resulting from epidemiological, cancer cell line, human tissue and animal studies. The prostate expresses both estrogen receptor alpha (ERA) and estrogen receptor beta (ERB). Most evidence suggests that ERA mediates the harmful effects of estrogen in the prostate, whereas ERB is tumour suppressive, but trials of ERB-selective agents have not translated into improved clinical outcomes. The role of ERB in the prostate remains unclear and there is increasing evidence that isoforms of ERB may be oncogenic. Detailed study of ERB and ERB isoforms in the prostate is required to establish their cell-specific roles, in order to determine if therapies can be directed towards ERB-dependent pathways. In this review, we summarise evidence on the role of ERB in prostate cancer and highlight areas for future research.

Implications of estrogen receptor alpha and estrogen receptor beta for adipose tissue functions and cardiometabolic complications

2013 ◽  
Vol 15 (3) ◽  
Author(s):  
Hui Gao ◽  
Karin Dahlman-Wright
Keyword(s):  
Estrogen Receptor ◽  
Adipose Tissue ◽  
Estrogen Receptor Alpha ◽  
Molecular Mechanisms ◽  
Estrogen Receptor Beta ◽  
Estrogen Receptor Α ◽  
Endocrine Function ◽  
Estrogen Signaling ◽  
Strongly Connected

AbstractThere is growing evidence that estrogen signaling regulates energy metabolism and exerts important functions in maintaining adipose tissue metabolism, including controlling the distribution of body fat. Changes in the physiological functions of adipose tissue, particularly the white adipose tissue, have been strongly connected to obesity and the development of related cardiometabolic complications. In this review, we will focus on discussing the role of estrogen signaling in regulating adipocyte differentiation, metabolism and its endocrine function with a focus on the possible underlying molecular mechanisms mediated by estrogen receptor α and estrogen receptor β.

scholarly journals Activation of estrogen response element dependent transcription by thyroid hormone with increase in estrogen receptor levels in a rat pituitary cell line, GH3

2004 ◽  
Vol 181 (1) ◽  
pp. 77-83 ◽  
Author(s):  
N Fujimoto ◽  
N Jinno ◽  
S Kitamura
Keyword(s):  
Estrogen Receptor ◽  
Thyroid Hormone ◽  
Cell Line ◽  
Estrogen Receptor Alpha ◽  
Hormone Receptors ◽  
Target Genes ◽  
Progesterone Receptors ◽  
Pituitary Cell ◽  
Gh3 Cells

Interrelationships between thyroid hormone and estrogen actions have been documented with regard to a variety of physiological functions. Both hormones stimulate transcription of target genes by binding to their nuclear receptors that interact with specific responsive elements (estrogen and thyroid hormone response elements, i.e ERE and TRE, respectively) in the regulatory regions of the gene. In vitro studies have suggested that interplay between the two hormones might be due to cross-talk at hormone responsive elements, with the respective hormone receptors and ligands able to interact, although physiological relevance has yet to be proved. We have proposed a simpler mechanism for thyroid hormone effects on estrogen responses via increase in estrogen receptor alpha (ERalpha) with resultant increase in progesterone receptors, prolactin production and tumor growth. A pituitary cell line, GH3, has been widely used to investigate the function of mammo-somatotropic cells, especially regarding regulation of GH and prolactin production. In the present study, an ERE-luc reporter was transfected into GH3 cells and the responses to endogenous ERalpha were examined. We demonstrated that: (1)l -3,5,3'-triiodothyronine (T3) induces mRNA expression of ERalpha; (2) T3 alone is able to induce ERE-luc activity and this is inhibited by OH-tamoxifen; (3) T3 synergistically acts on estradiol (E2)-induced ERE responses; and (4) ERE-luc activity is enchanted by co-transfection of an ERalpha expression vector. These results support the hypothesis that estrogen responses are potentiated by T3 through up-regulation of ERalpha levels.

scholarly journals 3,3′-Diindolylmethane Dose-Dependently Prevents Advanced Prostate Cancer

2019 ◽  
Author(s):  
Yufei Li ◽  
Nathaniel W. Mahloch ◽  
Nicholas J.E. Starkey ◽  
Mónica Peña-Luna ◽  
George E. Rottinghaus ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Estrogen Receptor ◽  
High Fat Diet ◽  
Estrogen Receptor Alpha ◽  
Estrogen Receptor Beta ◽  
Control Group ◽  
High Fat ◽  
Mouse Prostate

Abstract3,3′-Diindolylmethane (DIM) is an acid-derived dimer of indole-3-carbinol, found in many cruciferous vegetables, such as broccoli, and has been shown to inhibit prostate cancer (PCa) in several in vitro and in vivo models. We demonstrated that DIM stimulated both estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) transcriptional activities and propose that ERβ plays a role in mediating DIM’s inhibition on cancer cell growth. To further study the effects of DIM on inhibiting advanced PCa development, we tested DIM in TRAMP (TRansgenic Adenocarcinoma of the Mouse Prostate) mice. The control group of mice were fed a high fat diet. Three additional groups of mice were fed the same high fat diet supplemented with 0.04%, 0.2% and 1% DIM. Incidence of advanced PCa, poorly differentiated carcinoma (PDC), in the control group was 60%. 1% DIM dramatically reduced PDC incidence to 24% (p=0.0012), while 0.2% and 0.04% DIM reduced PDC incidence to 38% (p=0.047) and 45% (p=0.14) respectively. Though DIM did affect mice weights, statistical analysis showed a clear negative association between DIM concentration and PDC incidence with p=0.004, while the association between body weight and PDC incidence was not significant (p=0.953). In conclusion, our results show that dietary DIM can inhibit the most aggressive stage of prostate cancer at concentration lower than previously demonstrated, possibly working through an estrogen receptor mediated mechanism.

scholarly journals The Evaluation of Estrogen Receptor β as a Potential Prognosis Factor in Melanoma

2020 ◽  
Vol 70 (12) ◽  
pp. 4212-4216 ◽  
Keyword(s):  
Estrogen Receptor ◽  
Cutaneous Melanoma ◽  
Protective Factor ◽  
Hormone Receptors ◽  
Estrogen Receptor Beta ◽  
Prognostic Indicator ◽  
Sex Hormone ◽  
Estrogen Receptor Β ◽  
Keywords Melanoma ◽  
Receptor Beta

Differences across sexes in cutaneous melanoma incidence, metastatic pathways and disease outcome are consistently observed, with women having a significant survival advantage compared with men. This suggests that gender could play a role as a prognostic indicator through sex hormone signaling, but the mechanism is still unclear. This article focuses on available literature data concerning the influence of estrogen receptor beta (ERβ) expression as a host-related biological protective factor for female patients with melanoma. Furthermore, it highlights the potential role of estrogen receptor beta (ERβ) as a prognostic biologic marker in cutaneous melanoma. Keywords: melanoma, sex, hormone receptors, estrogen receptor β

scholarly journals Selective estrogen receptor modulators (SERMS)

2006 ◽  
Vol 50 (4) ◽  
pp. 720-734 ◽  
Author(s):  
Adolfo Diez-Perez
Keyword(s):  
Breast Cancer ◽  
Central Nervous System ◽  
Nervous System ◽  
Estrogen Receptor ◽  
Bone Density ◽  
Bone Turnover ◽  
Estrogen Receptor Alpha ◽  
Turnover Rate ◽  
Hormone Receptors ◽  
Estrogen Receptor Beta

Hormone receptors and, specifically, estrogen receptors were described about four decades ago. For estrogens, there are two receptors, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta). The two receptors are coded by different genes and their tissue expression varies across organs. ERalpha is predominantly expressed in reproductive tissues (uterus, breast, ovaries) liver and central nervous system, whereas ERbeta is expressed in other tissues such as bone, endothelium, lungs, urogenital tract, ovaries, central nervous system and prostate. More than seventy molecules that belong to the SERMS class have been described. There are 5 chemical groups: triphenylethylenes, benzotiophenes, tetrahydronaphtylenes, indoles and benzopyrans. All of these non-hormonal compounds are capable of activating the ER, reduce bone turnover rate and, as an antiresorptive, clearly improve bone density. Estrogens reduce bone turnover rate and, as an antiresorptive, clearly improve bone density. They are also beneficial for the relief of menopausal symptoms. An ongoing debate that extends over the decades, relates to to overall benefit/risk profile of estrogen or estrogen-progestin therapy since these therapies can increase the risk of serious health disorders, such as breast cancer. SERMs have increased our understanding of hormone-receptor regulatory mechanisms. Their development has permitted a targeted efficacy profile avoiding some of the side effects of the hormone therapy. Their clinical utility relies today mostly on the effects on breast cancer and bone.

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