{"title":"Targeted Imaging of Estrogen Receptor-Positive Cancer Cells Using Fluorescent Estradiol Probes","authors":"Shabnam Mansuri, Subhadra Ojha, Sriram Kanvah","doi":"10.1002/adom.202402758","DOIUrl":null,"url":null,"abstract":"<p>Breast cancer remains the second most common cause of cancer-related deaths in women worldwide, with ≈70% of cases linked to the overexpression of Estrogen Receptor (ERα). Existing imaging tools often fail to reliably differentiate between ER-positive and ER-negative cancer cells. To address this limitation, two novel fluorescent probes, <b>E2N</b> and <b>E2R</b>, are synthesized by conjugating estradiol to styryl and rhodamine-based fluorophores using click chemistry. These probes are characterized by their photophysical properties, biocompatibility, and selective targeting of ER-positive cells. Cellular uptake studies demonstrate preferential internalization of <b>E2N</b> and <b>E2R</b> in ER-positive MCF-7, ZR-75-1, and T-47D cells, with minimal uptake in ER-negative MDA-MB-231, MDA-MB-468, and healthy COS-7 and NIH-3T3 cell lines. Kinetic studies reveal efficient and rapid uptake of <b>E2N</b> in ER-positive MCF-7 cells, while mechanistic investigations identified clathrin-mediated endocytosis as the receptor-mediated pathway for both probes. Localization studies further confirm their mitochondrial specificity in ER-positive cells, with <b>E2R</b> displaying higher mitochondrial selectivity. These findings underscore the potential of <b>E2N</b> and <b>E2R</b> as powerful tools for distinguishing ER-positive from ER-negative breast cancer cells. Their receptor-mediated targeting and precise imaging capabilities make them promising candidates for advancing breast cancer diagnostics and enabling more targeted therapeutic strategies.</p>","PeriodicalId":116,"journal":{"name":"Advanced Optical Materials","volume":"13 8","pages":""},"PeriodicalIF":8.0000,"publicationDate":"2025-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Advanced Optical Materials","FirstCategoryId":"88","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/adom.202402758","RegionNum":2,"RegionCategory":"材料科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"MATERIALS SCIENCE, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
Abstract
Breast cancer remains the second most common cause of cancer-related deaths in women worldwide, with ≈70% of cases linked to the overexpression of Estrogen Receptor (ERα). Existing imaging tools often fail to reliably differentiate between ER-positive and ER-negative cancer cells. To address this limitation, two novel fluorescent probes, E2N and E2R, are synthesized by conjugating estradiol to styryl and rhodamine-based fluorophores using click chemistry. These probes are characterized by their photophysical properties, biocompatibility, and selective targeting of ER-positive cells. Cellular uptake studies demonstrate preferential internalization of E2N and E2R in ER-positive MCF-7, ZR-75-1, and T-47D cells, with minimal uptake in ER-negative MDA-MB-231, MDA-MB-468, and healthy COS-7 and NIH-3T3 cell lines. Kinetic studies reveal efficient and rapid uptake of E2N in ER-positive MCF-7 cells, while mechanistic investigations identified clathrin-mediated endocytosis as the receptor-mediated pathway for both probes. Localization studies further confirm their mitochondrial specificity in ER-positive cells, with E2R displaying higher mitochondrial selectivity. These findings underscore the potential of E2N and E2R as powerful tools for distinguishing ER-positive from ER-negative breast cancer cells. Their receptor-mediated targeting and precise imaging capabilities make them promising candidates for advancing breast cancer diagnostics and enabling more targeted therapeutic strategies.
期刊介绍:
Advanced Optical Materials, part of the esteemed Advanced portfolio, is a unique materials science journal concentrating on all facets of light-matter interactions. For over a decade, it has been the preferred optical materials journal for significant discoveries in photonics, plasmonics, metamaterials, and more. The Advanced portfolio from Wiley is a collection of globally respected, high-impact journals that disseminate the best science from established and emerging researchers, aiding them in fulfilling their mission and amplifying the reach of their scientific discoveries.