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Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
Published on: March 17, 2016
Estrogen related receptor α (ERRα) a promising target for the therapy of adrenocortical carcinoma (ACC)
Ivan Casaburi1, Paola Avena1, Arianna De Luca1
1Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Italy.
Abstract:
The pathogenesis of the adrenocortical cancer (ACC) involves integration of molecular signals and the interplay of different downstream pathways (i.e. IGFII/IGF1R, β-catenin, Wnt, ESR1). This tumor is characterized by limited therapeutic options and unsuccessful treatments. A useful strategy to develop an effective therapy for ACC is to identify a common downstream target of these multiple pathways. A good candidate could be the transcription factor estrogen-related receptor alpha (ERRα) because of its ability to regulate energy metabolism, mitochondrial biogenesis and signalings related to cancer progression. In this study we tested the effect of ERRα inverse agonist, XCT790, on the proliferation of H295R adrenocortical cancer cell line. Results from in vitro and in vivo experiments showed that XCT790 reduced H295R cell growth. The inhibitory effect was associated with impaired cell cycle progression which was not followed by any apoptotic event. Instead, incomplete autophagy and cell death by a necrotic processes, as a consequence of the cell energy failure, induced by pharmacological reduction of ERRα was evidenced. Our results indicate that therapeutic strategies targeting key factors such as ERRα that control the activity and signaling of bioenergetics processes in high-energy demanding tumors could represent an innovative/alternative therapy for the treatment of ACC.
Insights
Targeting estrogen-related receptor alpha (ERRα) with XCT790 inhibits adrenocortical cancer (ACC) cell growth. This approach disrupts cell energy, leading to necrosis and offering a potential new therapy for ACC.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Adrenocortical cancer (ACC) pathogenesis involves complex molecular signaling pathways.
- Current ACC treatments offer limited efficacy, necessitating novel therapeutic strategies.
- Estrogen-related receptor alpha (ERRα) regulates key cellular processes relevant to cancer progression.
Purpose of the Study:
- To investigate the therapeutic potential of targeting ERRα in ACC.
- To evaluate the effect of the ERRα inverse agonist XCT790 on ACC cell proliferation.
Main Methods:
- In vitro studies using the H295R adrenocortical cancer cell line.
- In vivo experiments to assess the efficacy of XCT790.
- Analysis of cell cycle progression, apoptosis, autophagy, and cell death mechanisms.
Main Results:
- XCT790 significantly reduced H295R cell growth in vitro and in vivo.
- Inhibition of cell cycle progression was observed, without significant apoptosis.
- Pharmacological reduction of ERRα led to incomplete autophagy, energy failure, and necrotic cell death.
Conclusions:
- Targeting ERRα with inverse agonists like XCT790 represents a promising therapeutic strategy for ACC.
- Disrupting ERRα-mediated bioenergetics pathways offers an innovative approach to ACC treatment.
- ERRα is a key regulator of energy metabolism and a potential target for novel ACC therapies.
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