Antiestrogens: structure-activity relationships and use in breast cancer treatment

Traboulsi, Tatiana; Ezzy, Mohamed El; Gleason, James L.; Mader, Sylvie

doi:10.1530/jme-16-0024

Cited by 68 publications

(65 citation statements)

References 148 publications

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“…Because the expression of CYP1A1 was also induced by DMSO at 3 and 9 h, TCDD or E2‐induced alteration in the mRNA expression levels of CYP1A1 was compared with DMSO treatment at each time point. In the cotreatment of ICI 182,780, which enhances ERα post‐translational modification by ubiquitin‐like molecules and accelerates its proteasomal degradation, E2‐induced mRNA expression levels increased in the expression of CYP1A1 mRNA at 24 h was reversed to the control level (Figure ). These results indicate that E2 induced the increase in mRNA expression levels of CYP1A1 like TCDD via ER dependent pathway.…”

Section: Resultsmentioning

confidence: 98%

Effect of dioxin and 17β-estradiol on the expression of cytochrome P450 1A1 gene via an estrogen receptor dependent pathway in cellular and xenografted models

Hwang

Kim

et al. 2017

Environmental Toxicology

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Cytochrome P450 (CYP) 1A1 plays a major role in the metabolic activation of procarcinogens to carcinogens via aryl hydrocarbon receptor (AhR) pathway. Especially, 2,3,7,8‐tetrachlorodibenzo‐p‐dioxin (TCDD) is known as an agonist of AhR. In estrogen responsive cancers, 17β‐estradiol (E2) may influence on AhR dependent expression of CYP1 family via the interaction between estrogen receptor (ER) and AhR. In the present study, the effect of E2/ER on the expression of AhR and CYP1A1 genes was investigated for MCF‐7 clonal variant (MCF‐7 CV) breast cancer cells expressing ER. In reverse transcription‐PCR and Western blot analysis, mRNA expression level of AhR was not altered, but its protein expression level was increased by TCDD or E2. The transcriptional and translational levels of CYP1A1 appeared to be increased by TCDD or E2. The increased expression of AhR and CYP1A1 induced by E2 was restored to the control level by the co‐treatment of ICI 182,780, indicating that E2 induced the protein expression levels of AhR and CYP1A1 like TCDD via an ER dependent pathway. In an in vivo xenograft mouse model transplanted with MCF‐7 CV cells, the protein expression levels of AhR and CYP1A1 of tumor masses were also increased by E2 or TCDD. Taken together, these results indicate that E2 may promote AhR dependent expression of CYP1A1 via ER dependent pathway in MCF‐7 CV cells expressing ER in the absence of TCDD, an agonist of AhR. The relevance of E2 and ER in CYP1A1 activation of estrogen responsive cancers may be targeted for developing more effective cancer treatments.

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Section: Resultsmentioning

confidence: 98%

Effect of dioxin and 17β-estradiol on the expression of cytochrome P450 1A1 gene via an estrogen receptor dependent pathway in cellular and xenografted models

Hwang

Kim

et al. 2017

Environmental Toxicology

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“…Consistent with the favorable safety profile of tamoxifen in humans, we did not observe adverse events with a short‐term administration. Reported adverse effects after prolonged use include endometrial cancers and thromboembolic accidents . The refractory hypocalcemic and hypomagnesemic tetany observed in a dexamethasone treated horse was associated with the loss of principal cells in the parathyroid gland which possibly decreased the production of parathyroid hormone.…”

Section: Discussionmentioning

confidence: 99%

“…Tamoxifen is a synthetic selective estrogen receptor modulator. Because of its antagonism of estrogen‐dependent growth and its inhibitory effect on breast epithelial cells proliferation, its major use has been in the treatment of breast cancer . Nonetheless, tamoxifen appears to have a broader spectrum of activity as it showed beneficial effects in estrogen‐receptor negative cancers, in selected immune disorders, and potentially in spinal cord injury .…”

Section: Introductionmentioning

confidence: 99%

Efficacy of tamoxifen for the treatment of severe equine asthma

Mainguy-Seers

Picotte

Lavoie

2018

Veterinary Internal Medicne

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BackgroundTamoxifen, a selective estrogen receptor modulator, decreased airway neutrophilia and improved clinical signs in an experimental model of equine asthma, and induced neutrophilic apoptosis in vitro.Hypothesis/ObjectivesTamoxifen reduces airway neutrophilia and improves lung function in severe asthmatic horses.AnimalsTwelve severe asthmatic horses from a research herd.MethodsRandomized controlled blinded study design. The effects of a 12‐day oral treatment with tamoxifen (0.22 mg/kg, q24h) or dexamethasone (0.06 mg/kg, q24h) on lung function, endoscopic tracheal mucus score and bronchoalveolar lavage fluid cytology were compared.ResultsTamoxifen significantly improved the pulmonary resistance (R L; mean reduction of 1.15 cm H2O/L/s [CI: 0.29‐2.01, P = .007] on day 13), but had no effect on the other variables evaluated. Dexamethasone normalized lung function (mean reduction of R L of 2.48 cm H2O/L/s [CI: 1.54‐3.43, P < .0001] on day 13), without affecting airway neutrophilia.Conclusions and Clinical ImportanceResults of this study do not support the use of tamoxifen at the dose studied as an antineutrophilic medication in the treatment of asthmatic horses in chronic exacerbation.

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“…Many diterpenoid alkaloids tend to exhibit improved activity after simple structural modification [58], and many structures may affect the activity of a compound, such as the kind and position of substituents and the linker-chain length [59]. …”

Section: Discussionmentioning

confidence: 99%

Anticancer Activities of C18-, C19-, C20-, and Bis-Diterpenoid Alkaloids Derived from Genus Aconitum

Ren

Shi

et al. 2017

Molecules

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Cancer is one of the most common lethal diseases, and natural products have been extensively studied as anticancer agents considering their availability, low toxicity, and economic affordability. Plants belonging to the genus Aconitum have been widely used medically in many Asian countries since ancient times. These plants have been proven effective for treating several types of cancer, such as lung, stomach, and liver cancers. The main effective components of Aconitum plants are diterpenoid alkaloids—which are divided into C18-, C19-, C20-, and bis-diterpenoid alkaloids—are reportedly some of the most promising, naturally abundant compounds for treating cancer. This review focuses on the progress of diterpenoid alkaloids with different structures derived from Aconitum plants and some of their derivatives with potential anticancer activities. We hope that this work can serve as a reference for further developing Aconitum diterpenoid alkaloids as anticancer agents.

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Antiestrogens: structure-activity relationships and use in breast cancer treatment

Cited by 68 publications

References 148 publications

Effect of dioxin and 17β-estradiol on the expression of cytochrome P450 1A1 gene via an estrogen receptor dependent pathway in cellular and xenografted models

Effect of dioxin and 17β-estradiol on the expression of cytochrome P450 1A1 gene via an estrogen receptor dependent pathway in cellular and xenografted models

Efficacy of tamoxifen for the treatment of severe equine asthma

Anticancer Activities of C18-, C19-, C20-, and Bis-Diterpenoid Alkaloids Derived from Genus Aconitum

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