New insights into the efficacy of <scp>SR</scp>‐16234, a selective estrogen receptor modulator, on the growth of murine endometriosis‐like lesions

Khine, Yin Mon; Taniguchi, Fuminori; Nagira, Keita; Nakamura, Kazuomi; Ohbayashi, Tetsuya; Osaki, Mitsuhiko; Harada, Tasuku

doi:10.1111/aji.13023

Cited by 10 publications

(8 citation statements)

References 39 publications

(76 reference statements)

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“…After one daily administration of bazedoxifene/conjugated estrogens for 12 weeks, all subjects demonstrated an LH surge without endometrial alterations or abnormal ovarian folliculogenesis [79]. Khine et al evaluated the effects of SR-16234 on murine endometriosis-like lesions [80]. SR-16234 is a SERM which was reported to have ERα-antagonistic activity with a weak partially agonist activity to the ERβ receptor.…”

Section: Treatments and Innovations In Clinical Management Related To Ersmentioning

confidence: 99%

Estrogen Receptors and Endometriosis

Chantalat

Valera

Vaysse

et al. 2020

IJMS

154

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Endometriosis is a frequent and chronic inflammatory disease with impacts on reproduction, health and quality of life. This disorder is highly estrogen-dependent and the purpose of hormonal treatments is to decrease the endogenous ovarian production of estrogens. High estrogen production is a consistently observed endocrine feature of endometriosis. mRNA and protein levels of estrogen receptors (ER) are different between a normal healthy endometrium and ectopic/eutopic endometrial lesions: endometriotic stromal cells express extraordinarily higher ERβ and significantly lower ERα levels compared with endometrial stromal cells. Aberrant epigenetic regulation such as DNA methylation in endometriotic cells is associated with the pathogenesis and development of endometriosis. Although there is a large body of data regarding ERs in endometriosis, our understanding of the roles of ERα and ERβ in the pathogenesis of endometriosis remains incomplete. The goal of this review is to provide an overview of the links between endometriosis, ERs and the recent advances of treatment strategies based on ERs modulation. We will also attempt to summarize the current understanding of the molecular and cellular mechanisms of action of ERs and how this could pave the way to new therapeutic strategies.

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Section: Treatments and Innovations In Clinical Management Related To Ersmentioning

confidence: 99%

Estrogen Receptors and Endometriosis

Chantalat

Valera

Vaysse

et al. 2020

IJMS

154

View full text Add to dashboard Cite

show abstract

“…Another recent study suggested dual targeting of ERα with tamoxifen and ERRα with XCT790 may be beneficial for EC treatment, but this requires further validation (Mao et al 2019). While administration of SERMs/SERDs may be appropriate for postmenopausal women with cancer, their use in younger women with non-malignant endometrial disorders such as endometriosis is more challenging with data limited to promising results in preclinical models (Kulak et al 2011, Khine et al 2018. The observation that ERβ is highly expressed in endometriosis lesions and the development of ERβ-selective agonists such as ERβ-041 with apparent anti-inflammatory properties provided a rationale for testing them as therapies for endometriosis with promising results obtained in preclinical models (Harris 2006).…”

Section: Targeting Oestrogen Receptors In Endometrial Disordersmentioning

confidence: 99%

Androgens, oestrogens and endometrium: a fine balance between perfection and pathology

Gibson

Simitsidellis

Collins

et al. 2020

Journal of Endocrinology

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The endometrium is a complex multicellular tissue that is exquisitely sensitive to the actions of sex steroids synthesised in the ovary (endocrine system). Recent studies have highlighted a previously under-appreciated role for local (intracrine) metabolism in fine-tuning tissue function in both health and disease. In this review we have focused on the impact of oestrogens and androgens on endometrial function summarising data from studies on normal endometrial physiology and disorders including infertility, endometriosis and cancer. We consider the evidence that expression of enzymes including aromatase, sulphatase and AKR1C3 by endometrial cells plays an important role in tissue function, and malfunction, and discus results from studies using drugs targeting intracrine pathways to treat endometrial disorders. We summarise studies exploring the spatial and temporal expression of oestrogen receptors (ERalpha, ERbeta and GPER) and their role in mediating the impact of endogenous and synthetic ligands on cross-talk between vascular, immune, epithelial and stromal cells. There is a single androgen receptor and androgens play a key role in stromal-epithelial cross talk, scar-free healing of endometrium during menstruation and regulation of cell proliferation. The development of new receptor-selective drugs (SERMs, SARMs, SARDs) has reinvigorated interest in targeting receptor subtypes in treatment of disorders including endometriosis and endometrial cancer and some show promise as novel therapies. In summary, understanding the mechanisms regulated by sex steroids provides the platform for improved personalised treatment of endometrial disorders as well as novel insights into the impact of steroids on processes such as tissue repair and regeneration.

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“…BALB/c mouse model [36] INT-777 Suppresses TGR5/TNFα/NF-κB pathway in endometriotic cells. hESCs isolated from patients with endometriosis [116] Niclosamide Inhibits macrophage-induced inflammation and endometriotic cell viability partly via suppressing NF-κB signaling.…”

Section: Preclinical Drugs For Blocking Nf-κb Signaling In Endometriosismentioning

confidence: 99%

Section: Regulation Of Nf-κb Signaling In Endometriosismentioning

confidence: 99%

“…SR-16234 is a selective estrogen receptor modulator that has potent antagonistic activity on ERα with weak partial agonist activity against the ERβ receptor 36 . In a BALB/c mouse model of endometriosis, treatment with SR-16234 substantially decreased NF-κB p65 expression and reduced the growth of endometriotic lesions 36 . In an open-label single-arm clinical trial, the oral administration of SR-16234 substantially relieved the pain symptoms of patients with endometriosis 37 .…”

Section: Regulation Of Nf-κb Signaling In Endometriosismentioning

confidence: 99%

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An Update on the Multifaceted Role of NF-kappaB in Endometriosis

2022

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Endometriosis remains a common but challenging gynecological disease among reproductive-aged women with an unclear pathogenesis and limited therapeutic options. Numerous pieces of evidence suggest that NF-κB signaling, a major regulator of inflammatory responses, is overactive in endometriotic lesions and contributes to the onset, progression, and recurrence of endometriosis. Several factors, such as estrogen, progesterone, oxidative stress, and noncoding RNAs, can regulate NF-κB signaling in endometriosis. In the present review, we discuss the mechanisms by which these factors regulate NF-κB during endometriosis progression and provide an update on the role of NF-κB in affecting endometriotic cells, peritoneal macrophages (PMs) as well as endometriosis-related symptoms, such as pain and infertility. Furthermore, the preclinical drugs for blocking NF-κB signaling in endometriosis are summarized, including plant-derived medicines, NF-κB inhibitors, other known drugs, and the potential anti-NF-κB drugs predicted through the Drug-Gene Interaction Database. The present review discusses most of the studies concerning the multifaceted role of NF-κB signaling in endometriosis and provides a summary of NF-κB-targeted treatment in detail.

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New insights into the efficacy of SR‐16234, a selective estrogen receptor modulator, on the growth of murine endometriosis‐like lesions

Abstract: SR has a regressive effect on the development of murine endometriosis-like lesions.

Cited by 10 publications

References 39 publications

Estrogen Receptors and Endometriosis

Estrogen Receptors and Endometriosis

Androgens, oestrogens and endometrium: a fine balance between perfection and pathology

An Update on the Multifaceted Role of NF-kappaB in Endometriosis

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