Dai Junhong, Wu Yihe, Deng Xiaofei, Zhou Hai-Bing, Dong Chune
Department of Gynecological Oncology, Zhongnan Hospital of Wuhan University, School of Pharmaceutical Sciences, Wuhan University Wuhan 430071 China
State Key Laboratory of Virology, Frontier Science Center for Immunology and Metabolism, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University), Ministry of Education, Wuhan University Wuhan 430071 China.
RSC Med Chem. 2024 Dec 11. doi: 10.1039/d4md00767k.
Estrogen receptor β (ERβ) is aberrantly expressed in castration-resistant prostate cancer (CRPC). Therefore, a diagnostic and therapeutic ERβ probe not only helps to reveal the complex role of ERβ in prostate cancer (PCa), but also promotes ERβ-targeted PCa therapy. Herein, we reported a novel ERβ-targeted near-infrared fluorescent probe D3 with both imaging and therapeutic functions, which had the advantages of high ERβ selectivity, good optical performance, and strong anti-interference ability. In addition, it displayed excellent antiproliferative activity in CRPC cells. Finally, D3 was also successfully applied to the imaging of ERβ in the prostate cancer mouse model. Thus, this ERβ-targeted near-infrared fluorescent probe can be used as a potential tool for the study of ERβ-targeted diagnostic and therapeutic PCa.
雌激素受体β（ERβ）在去势抵抗性前列腺癌（CRPC）中异常表达。因此，一种诊断和治疗性的ERβ探针不仅有助于揭示ERβ在前列腺癌（PCa）中的复杂作用，还能促进针对ERβ的PCa治疗。在此，我们报道了一种新型的具有成像和治疗功能的靶向ERβ的近红外荧光探针D3，它具有ERβ选择性高、光学性能好和抗干扰能力强的优点。此外，它在CRPC细胞中表现出优异的抗增殖活性。最后，D3也成功应用于前列腺癌小鼠模型中ERβ的成像。因此，这种靶向ERβ的近红外荧光探针可作为研究针对ERβ的PCa诊断和治疗的潜在工具。
