2. Academic Validation
  3. Discovery of ERα-targeting PROTACs with intrinsic fluorescence for precision theranostics of breast cancer

Discovery of ERα-targeting PROTACs with intrinsic fluorescence for precision theranostics of breast cancer

  • RSC Med Chem. 2025 May 22. doi: 10.1039/d5md00281h.
Yihe Wu 1,  Junhong Dai 1,  Xiaofei Deng 1,  Pei He 1,  Jinsen Liang 1,  Lilan Xin 1,  Baohua Xie 1,  Shenghong Zhu 2,  Chune Dong 1,  Hai-Bing Zhou 1 3
Affiliations

Affiliations

  • 1 Department of Hematology, Zhongnan Hospital of Wuhan University, School of Pharmaceutical Sciences, Wuhan University Wuhan 430071 China cdong@whu.edu.cn zhouhb@whu.edu.cn.
  • 2 Yangtze River Pharmaceutical Group JiangSu Haici Biological Pharmaceutical Co., Ltd. 8 Taizhen Road, Medical New & Hi-tech Industrial Development Zone Taizhou 225321 China.
  • 3 State Key Laboratory of Virology and Biosafety, Frontier Science Center for Immunology and Metabolism, School of Pharmaceutical Sciences, Wuhan University Wuhan 430071 China.
PMID: 40530084 DOI: 10.1039/d5md00281h
Abstract

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 in vivo safety assay indicated that W2 was well-tolerated up to a dose of 500 mg kg-1 with no acute toxicity. This work demonstrates the great potential of ERα-targeted PROTACs as theranostic agents in breast Cancer treatment.

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