Long-term selective estrogen receptor-beta agonist treatment modulates gene expression in bone and bone marrow of ovariectomized rats

Balla, Bernadett; Sárvári, Miklós; Kósa, János P.; Kocsis-Deák, Barbara; Tobiás, Bálint; Árvai, Kristóf; Takács, István; Podani, János; Liposits, Zsolt; Lakatos, Péter

doi:10.1016/j.jsbmb.2019.01.012

Cited by 26 publications

(17 citation statements)

References 44 publications

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“…At present, the widespread expression of ERβ is detected not only in luminal and myoepithelial cells in the normal breast but also in subcutaneous adipose tissue [ 9 ] and prostate, testis, uterus, ovary, and brain tissues [ 10 ]. Alternations in estrogenic signaling pathways, as well as ERβ expression, have been discussed in the context of physiological and pathological processes, such as maintenance of the bone marrow microenvironment [ 11 ], neuronal-mediated contractions of the gastrointestinal tract [ 12 ], recovery of reproductive system injury [ 13 ], anxiolytic effects [ 14 ], and diseases such as Parkinson’s disease [ 15 ], endometriosis [ 16 ], myocardial infarction [ 17 ] and type 2 diabetes [ 18 ]. Moreover, ERβ has been shown to participate in the pathological process of various cancers, including uterine leiomyomas [ 19 ], colorectal cancer [ 20 ], desmoid tumors [ 21 ], prostate cancer [ 22 ] and duct carcinoma [ 23 ].…”

Section: Introductionmentioning

confidence: 99%

The role of estrogen receptor beta in breast cancer

Zhou

Liu

2020

Biomark Res

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Breast cancer, a malignant tumor originating from mammary epithelial tissue, is the most common cancer among women worldwide. Challenges facing the diagnosis and treatment of breast cancer necessitate the search for new mechanisms and drugs to improve outcomes. Estrogen receptor (ER) is considered to be important for determining the diagnosis and treatment strategy. The discovery of the second estrogen receptor, ERβ, provides an opportunity to understand estrogen action. The emergence of ERβ can be traced back to 1996. Over the past 20 years, an increasing body of evidence has implicated the vital effect of ERβ in breast cancer. Although there is controversy among scholars, ERβ is generally thought to have antiproliferative effects in disease progression. This review summarizes available evidence regarding the involvement of ERβ in the clinical treatment and prognosis of breast cancer and describes signaling pathways associated with ERβ. We hope to highlight the potential of ERβ as a therapeutic target.

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Section: Introductionmentioning

confidence: 99%

The role of estrogen receptor beta in breast cancer

Zhou

Liu

2020

Biomark Res

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“…The common expression of ERβ is detected in luminal and myoepithelial cells in the normal breast but also in subcutaneous adipose tissue [50] and testis, prostate, ovary, uterus, and brain tissues [51]. Changes in estrogenic signaling pathways have been discoursed in the physiological and pathological processes [52], neuronal-mediated contractions of the gastrointestinal tract [53], recovery of reproductive system injury [54], anxiolytic effects [55], and diseases such as Parkinson's disease [56] or endometriosis [57]. Furthermore, ERβ has been shown to take part in the pathological process of various cancers, e.g., colorectal cancer [58], prostate cancer [59] or duct carcinoma [60].…”

Section: Estrogen Receptormentioning

confidence: 99%

Steroid Receptors in Breast Cancer: Understanding of Molecular Function as a Basis for Effective Therapy Development

Kowalczyk

Waliszczak

Jach

et al. 2021

Cancers

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Breast cancer remains one of the most important health problems worldwide. The family of steroid receptors (SRs), which comprise estrogen (ER), progesterone (PR), androgen (AR), glucocorticoid (GR) and mineralocorticoid (MR) receptors, along with a receptor for a secosteroid—vitamin D, play a crucial role in the pathogenesis of the disease. They function predominantly as nuclear receptors to regulate gene expression, however, their full spectrum of action reaches far beyond this basic mechanism. SRs are involved in a vast variety of interactions with other proteins, including extensive crosstalk with each other. How they affect the biology of a breast cell depends on such factors as post-translational modifications, expression of coregulators, or which SR isoform is predominantly synthesized in a given cellular context. Although ER has been successfully utilized as a breast cancer therapy target for years, research on therapeutic application of other SRs is still ongoing. Designing effective hormone therapies requires thorough understanding of the molecular function of the SRs. Over the past decades, huge amount of data was obtained in multiple studies exploring this field, therefore in this review we attempt to summarize the current knowledge in a comprehensive way.

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“…In addition to presenting in mammary epithelial and ductal cells, ERβ is detected in various tissues, such as subcutaneous adipose tissue [5], brain, and prostate [6]. Furthermore, changes in ERβ expression levels and downstream pathways are involved in regulating many physiological and pathological processes [7][8][9], such as the occurrence and development of the Parkinson's disease [10],…”

Section: Introductionmentioning

confidence: 99%

Development of a Novel 18F-labeled Probe for PET imaging of Estrogen Receptor β

Zhou

Peng

Han

et al. 2022

Preprint

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Purpose: Estrogen receptors beta (ERβ) is an important ER subtype and plays crucial roles in many physiological and pathological disorders. Herein, we aim to develop a probe, 18F-PVBO, for in vivo ERβ targeted PET imaging with promising results.Methods: 18F-PVBO was synthesized using a two-step radiolabeling method. The relative binding affinities of the reference compound PVBO towards ERα and ERβ were determined by a competitive radiometric binding assay using 3H-estradiol. Cytotoxicity and cell uptake were evaluated in ERβ-positive DU145 cells. PET imaging, including blocking study, was performed in DU145 tumor-bearing nude mice (n = 3 per group), and the biodistribution study of 18F-PVBO was also performed.Results: The non-radioactive PVBO showed 12.46-fold stronger binding affinity to ERβ than to ERα in vitro. 18F-PVBO was synthesized with a 15-28% radiochemical yield (n = 5) within 40 min, and the radiochemical purity was >98%. The uptake of 18F-PVBO in DU145 cells was significantly blocked by ERB-041 (p < 0.05). The uptake of 18F-PVBO in DU145 xenografts increased during the 120 min dynamic scanning, with a maximum uptake of 2.80 ± 0.30% ID/g at 120 min. Based on time active curves (TACs), injection of 18F-PVBO with unlabeled PVBO or ERB-041 resulted in a significant signals reduction with the T/M ratio <1 at 30, 60, 75, and 120 min post-injection (p <0.05). Comparison of the %ID/g showed 18F-PVBO had a higher T/M ratio compared to 18F-FES in DU145 tumor-bearing mice at 60 min (1.65 vs. 1.28), 75 min (1.76 vs. 1.35), and 120 min (1.80 vs. 1.37) (p < 0.05). Conclusion: 18F-PVBO shows 12.46-fold stronger binding to ERβ over ERα, with high radiochemical stability. It demonstrates the feasibility of noninvasively imaging ERβ positive tumors by small-animal PET and provides a new strategy for visualizing of ERβ in vivo.

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Long-term selective estrogen receptor-beta agonist treatment modulates gene expression in bone and bone marrow of ovariectomized rats

Cited by 26 publications

References 44 publications

The role of estrogen receptor beta in breast cancer

The role of estrogen receptor beta in breast cancer

Steroid Receptors in Breast Cancer: Understanding of Molecular Function as a Basis for Effective Therapy Development

Development of a Novel 18F-labeled Probe for PET imaging of Estrogen Receptor β

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