Size, site, and signaling: Three attributes of estrogen receptors

Desouza, Junita; Gadkar, Sushama; Jagtap, Dhanashree D.; Sachdeva, Geetanjali

doi:10.4103/bmrj.bmrj_24_19

Cited by 2 publications

(3 citation statements)

References 114 publications

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“…A novel splice variant of the human ERa, ERa30, was recently identified and cloned from clinical breast cancer tissue (20). The ERa-30 sequence lacks an LBD and a liganddependent transcriptional activation domain but retains the Nterminal transcriptional activation domain, the DBD, a partial hinge domain and possesses a unique 10-aminoacid domain.…”

Section: Splice Variants In the Estrogen Receptormentioning

confidence: 99%

“…The ERa-30 sequence lacks an LBD and a liganddependent transcriptional activation domain but retains the Nterminal transcriptional activation domain, the DBD, a partial hinge domain and possesses a unique 10-aminoacid domain. Nonetheless, different isoforms are generated not only by alternative splicing but also through post-transcriptional modifications (20).…”

Section: Splice Variants In the Estrogen Receptormentioning

confidence: 99%

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Distribution and Effects of Estrogen Receptors in Prostate Cancer: Associated Molecular Mechanisms

et al. 2022

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Estrogens are hormones that have been extensively presented in many types of cancer such as breast, uterus, colorectal, prostate, and others, due to dynamically integrated signaling cascades that coordinate cellular growth, differentiation, and death which can be potentially new therapeutic targets. Despite the historical use of estrogens in the pathogenesis of prostate cancer (PCa), their biological effect is not well known, nor their role in carcinogenesis or the mechanisms used to carry their therapeutic effects of neoplastic in prostate transformation. The expression and regulation of the estrogen receptors (ERs) ERα, ERβ, and GPER stimulated by agonists and antagonists, and related to prostate cancer cells are herein reviewed. Subsequently, the structures of the ERs and their splice variants, the binding of ligands to ERs, and the effect on PCa are provided. Finally, we also assessed the contribution of molecular simulation which can help us to search and predict potential estrogenic activities.

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Section: Splice Variants In the Estrogen Receptormentioning

confidence: 99%

Section: Splice Variants In the Estrogen Receptormentioning

confidence: 99%

Distribution and Effects of Estrogen Receptors in Prostate Cancer: Associated Molecular Mechanisms

et al. 2022

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“…Full-length ERα and ERβ are reported to be expressed in various tissues. Estrogen receptors (ERs) have been found to localize to the nucleus, mitochondria, and plasma membrane (around 5%-10% of the population) [19]. ERs have also been found in discrete cytoplasmic organelles, such as the endoplasmic reticulum [20].…”

Section: Introductionmentioning

confidence: 99%

Isolation and Characterization of Phenylpropanoid and Lignan Compounds from Peperomia pellucida [L.] Kunth with Estrogenic Activities

et al. 2020

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Extracts of Peperomia pellucida [L.] Kunth have previously been demonstrated to have in vivo estrogenic-like effects, thereby functioning as an anti-osteoporotic agent. However, the compounds responsible for these effects have not yet been determined. Therefore, the aim of this study is to isolate and elucidate potential compounds with estrogenic activity. The structures of the isolated compounds were identified using 1D 1H and 13C-NMR and confirmed by 2D FT-NMR. The estrogenic activity was evaluated using the E-SCREEN assay, and a molecular docking study was performed to predict the binding affinity of the isolated compounds to estrogen receptors. In this experiment, we successfully isolated three phenylpropanoids and two lignan derivatives, namely, 6-allyl-5-methoxy-1,3-benzodioxol-4-ol (1), pachypostaudin B (2), pellucidin A (3), dillapiole (4), and apiol (5). Among these compounds, the isolation of 1 and 2 from P. pellucida is reported for the first time in this study. Activity assays clearly showed that the ethyl acetate extract and its fractions, subfractions, and isolated compounds exerted estrogenic activity. Methanol fraction of the ethyl acetate extract produced the highest estrogenic activity, while 1 and 2 had partial agonist activity. Some compounds (derivates of dillapiole and pellucidin A) also had, in addition, anti-estrogenic activity. In the docking study, the estrogenic activities of 1–5 appeared to be mediated by a classical ligand-dependent mechanism as suggested by the binding interaction between the compounds and estrogen receptors; binding occurred on Arg 394 and His 524 of the alpha receptor and Arg 346 and His 475 of the beta receptor. In summary, we reveal that P. pellucida is a promising anti-osteoporotic agent due to its estrogenic activity, and the compounds responsible for this activity were found to be lignan and phenylpropanoid derivatives. The presence of other compounds in either the extract or fraction may contribute to a synergistic effect, as suggested by the higher estrogenic activity of the methanol fraction. Hence, we suggest further research on the osteoporotic activity and safety of the identified compounds, especially regarding their effects on estrogen-responsive organs.

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Size, site, and signaling: Three attributes of estrogen receptors

Cited by 2 publications

References 114 publications

Distribution and Effects of Estrogen Receptors in Prostate Cancer: Associated Molecular Mechanisms

Distribution and Effects of Estrogen Receptors in Prostate Cancer: Associated Molecular Mechanisms

Isolation and Characterization of Phenylpropanoid and Lignan Compounds from Peperomia pellucida [L.] Kunth with Estrogenic Activities

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