Synthesis and preliminary evaluation of a PET-FI bimodal imaging agent targeting estrogen receptor

Estrogen receptor is an attractive target for the diagnosis and treatment of breast cancer. This article reports for the first time a dual-modality imaging agent targeting estrogen receptor that can use PET imaging to diagnose breast cancer and utilize fluorescence imaging to achieve intraoperative navigation. Fluorescence experiments show that [^natGa] 1 has typical aggregate induced emission characteristics. Above the critical concentration, [^natGa] 1 can form biocompatible nanomicelles. [^natGa] 1 can quickly light up estrogen receptor positive MCF-7 cells. Cell uptake experiments show that [⁶⁸Ga] 1 is mediated by estrogen receptor. Therefore, [^nat/68Ga] 1 shows the characteristics of highly sensitive diagnosis and visualization of breast cancer, and can be used as a lead compound for the development of a novel PET-FI bimodal imaging agent targeting the estrogen receptor.