{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,31]],"date-time":"2026-10-31T17:25:24Z","timestamp":1793467524181,"version":"4.5.0"},"reference-count":426,"publisher":"Frontiers Media SA","license":[{"start":{"date-parts":[[2025,6,26]],"date-time":"2025-06-26T00:00:00Z","timestamp":1750896000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":["frontiersin.org"],"crossmark-restriction":true},"short-container-title":["Front. Oncol."],"abstract":"<jats:p>\n                    Classical estrogen receptors, ER\u03b1 and ER\u03b2, along with the membrane-bound G-protein-coupled estrogen receptor (GPER), play critical roles in driving ER\u03b1\u2212positive breast cancer (BC). Clinical management of this subtype relies on endocrine therapy (ET), which targets ER signaling through selective estrogen receptors modulators (SERMs), degraders (SERDs), and aromatase inhibitors (AIs). While ET has significantly reduced recurrence and mortality rates, acquired resistance remains a major therapeutic challenge. Activating\n                    <jats:italic>ESR1<\/jats:italic>\n                    mutations, which encode constitutively active ER\u03b1 variants, are detected in 30-50% of therapy-resistant metastatic ER\u03b1\u2212positive BC and serve as emerging biomarkers of poor prognosis. These hot-spot mutations stabilize ER\u03b1 in its agonist conformation, thereby enabling ligand-independent transcriptional activation. Understanding the conformational constraints that keep wild-type ER\u03b1 in an \u201coff-state\u201d in the absence of ligand\u2014and how activating\n                    <jats:italic>ESR1<\/jats:italic>\n                    mutations disrupt these regulatory mechanisms\u2014is critical for developing effective targeted therapies. Concurrently, GPER-mediated non-genomic signaling, often inadvertently activated by SERMs and SERDs, contributes to tamoxifen resistance. This review explores the structural and functional intricacies of ER\u03b1, the impact of\n                    <jats:italic>ESR1<\/jats:italic>\n                    mutations on its ligand-binding domain (ER\u03b1\u2212LBD) and their contribution to ET resistance, and the role of GPER-mediated signaling in ER\u03b1\u2212positive BC. We further highlight recent advances in next-generation therapeutics targeting both ER\u03b1 mutants and GPER, which may offer a more effective, integrated strategy to overcome ET resistance.\n                  <\/jats:p>","DOI":"10.3389\/fonc.2025.1513225","type":"journal-article","created":{"date-parts":[[2025,6,26]],"date-time":"2025-06-26T01:29:24Z","timestamp":1750901364000},"update-policy":"https:\/\/doi.org\/10.3389\/crossmark-policy","source":"Crossref","is-referenced-by-count":17,"title":["Decoding estrogen receptor and GPER biology: structural insights and therapeutic advances in ER\u03b1\u2212positive breast cancer"],"prefix":"10.3389","volume":"15","author":[{"given":"Taniya","family":"Saha","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kiven 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