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

Estrogen receptor beta (ER beta) is aberrantly expressed in castration-resistant prostate cancer (CRPC). Therefore, a diagnostic and therapeutic ER beta probe not only helps to reveal the complex role of ER beta in prostate cancer (PCa), but also promotes ER beta-targeted PCa therapy. Herein, we reported a novel ER beta-targeted near-infrared fluorescent probe D3 with both imaging and therapeutic functions, which had the advantages of high ER beta 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 in vivo imaging of ER beta in the prostate cancer mouse model. Thus, this ER beta-targeted near-infrared fluorescent probe can be used as a potential tool for the study of ER beta-targeted diagnostic and therapeutic PCa.