Selective Induction of Estrogen Receptor-Dependent Stress Signaling as a Therapeutic Strategy in Resistant Breast Cancer
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 models─offering a conceptually distinct strategy for overcoming endocrine resistance.
Authors
- Anna C. Renner (ORCID: https://orcid.org/0000-0003-4971-9609)
- Robert B. Kargbo (ORCID: https://orcid.org/0000-0002-5539-6343)
Institutions
- Dakota State University (US)
- North Dakota State University (US)
Publication Details
- Journal
- ACS Medicinal Chemistry Letters
- Published
- 2026-04-14
- DOI
- https://doi.org/10.1021/acsmedchemlett.6c00171
- Primary Topic
- Endoplasmic Reticulum Stress and Disease
- Type
- article
- Field-Weighted Citation Impact
- 0.00