发现er α-靶向本征荧光PROTACs用于乳腺癌的精准治疗。

IF 3.597 Q2 Pharmacology, Toxicology and Pharmaceutics

MedChemComm Pub Date : 2025-05-22 DOI:10.1039/D5MD00281H

Yihe Wu, Junhong Dai, Xiaofei Deng, Pei He, Jinsen Liang, Lilan Xin, Baohua Xie, Shenghong Zhu, Chune Dong and Hai-Bing Zhou

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引用次数: 0

摘要

实时监测蛋白质降解是一项挑战。本文设计并合成了具有本征荧光的新型er α靶向双功能PROTACs，用于乳腺癌的精准治疗。其中W2在MCF-7乳腺癌细胞系中表现出良好的抗增殖活性、选择性ERα降解和成像能力。体内安全性试验表明，W2耐受性良好，剂量达500 mg kg-1，无急性毒性。这项工作证明了er α-靶向PROTACs作为乳腺癌治疗药物的巨大潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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

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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 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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来源期刊

MedChemComm BIOCHEMISTRY & MOLECULAR BIOLOGY-CHEMISTRY, MEDICINAL

CiteScore

4.70

自引率

0.00%

发文量

审稿时长

2.2 months

期刊介绍： Research and review articles in medicinal chemistry and related drug discovery science; the official journal of the European Federation for Medicinal Chemistry. In 2020, MedChemComm will change its name to RSC Medicinal Chemistry. Issue 12, 2019 will be the last issue as MedChemComm.