Discovery of ERα-targeting PROTACs with intrinsic fluorescence for precision theranostics of breast cancer
Real-time monitoring of protein degradation is challenging. Herein, novel ERα-targeted dual-function PROTACs with intrinsic fluorescence were designed and synthesized for precision theranostics of breast cancer. Among them, W2 showed good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. The <i>in vivo</i> safety assay indicated that W2 was well-tolerated up to a dose of 500 mg kg<sup>-1</sup> with no acute toxicity. This work demonstrates the great potential of ERα-targeted PROTACs as theranostic agents in breast cancer treatment.
Authors
- Lilan Xin (ORCID: https://orcid.org/0000-0003-3889-4989)
- Xiaofei Deng (ORCID: https://orcid.org/0000-0001-6600-4918)
- Hai‐Bing Zhou (ORCID: https://orcid.org/0000-0001-8498-063X)
- Xie Baohua
- Chune Dong (ORCID: https://orcid.org/0000-0001-7651-7995)
- Shan Zhu (ORCID: https://orcid.org/0000-0003-1531-6174)
- Yihe Wu (ORCID: https://orcid.org/0000-0002-6331-5283)
- Junhong Dai
- Jinsen Liang
- Pei He
Institutions
- Wuhan University (CN)
- Zhongnan Hospital of Wuhan University (CN)
- Yangtze River Pharmaceutical Group (China) (CN)
Publication Details
- Journal
- RSC Medicinal Chemistry
- Published
- 2025-01-01
- DOI
- https://doi.org/10.1039/d5md00281h
- Primary Topic
- Protein Degradation and Inhibitors
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China