An estrogen receptor β‑targeted near-infrared probe for theranostic imaging of prostate cancer

Abstract

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 PC therapy. Herein, we reported a novel ERβ-targeted near-infrared fluorescent probe D3 with both imaging and therapeutic functions, which has 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 in vivo imaging of ERβ in the prostate cancer mice 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 PC.