Discovery of the ERα-Targeting PROTACs with Intrinsic Fluorescence for Precision Theranostics of Breast Cancer

Abstract

Real-time monitoring of protein degradation is challenging. Herein, the 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 various 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 with no acute toxicity. This work demonstrates the great potential of ERα-targeted PROTACs as the theranostic agents in breast cancer treatment.