关键词: Aggregate induced emission Bimodal imaging agent ER+ breast cancer Estrogen receptor PET

Mesh : Breast Neoplasms / diagnostic imaging Female Germanium / chemistry Humans Isotope Labeling MCF-7 Cells Molecular Conformation Optical Imaging Positron-Emission Tomography Radiopharmaceuticals / chemical synthesis chemistry Receptors, Estrogen / analysis

来  源:   DOI:10.1016/j.bmcl.2021.127776   PDF(Sci-hub)

Abstract:
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.
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