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Updated: May 21, 2026

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
Published on: March 17, 2016
Selective Induction of Estrogen Receptor-Dependent Stress Signaling as a Therapeutic Strategy in Resistant Breast
Anna C Renner1, Robert B Kargbo2
1North Dakota State University, Fargo, North Dakota 58108-6050, United States.
Abstract:
Estrogen receptor alpha (ERα) is the defining therapeutic target in hormone receptor-positive breast cancer, yet acquired resistance remains a persistent barrier to durable clinical benefit. Patent application WO 2026/039467 A1 discloses small molecules that activate an anticipatory unfolded protein response (a-UPR) through ERα, converting receptor engagement into selective cytotoxic stress. This mechanism diverges fundamentally from classical antagonism or degradation and demonstrates preferential activity in ERα-positive tumor modelsoffering a conceptually distinct strategy for overcoming endocrine resistance.
Insights
New small molecules activate estrogen receptor alpha (ERα) to induce a targeted cancer cell death pathway. This approach offers a novel strategy to overcome endocrine resistance in ERα-positive breast cancer.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Estrogen receptor alpha (ERα) is a key target in hormone receptor-positive breast cancer.
- Acquired resistance to endocrine therapies limits long-term patient benefit.
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