Synthesis And Preliminary Evaluation Of A Pet-Fi Bimodal Imaging Agent Targeting Estrogen Receptor
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(2021)
摘要
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 [Ga-nat] 1 has typical aggregate induced emission characteristics. Above the critical concentration, [Ga-nat] 1 can form biocompatible nanomicelles. [Ga-nat] 1 can quickly light up estrogen receptor positive MCF-7 cells. Cell uptake experiments show that [Ga-68] 1 is mediated by estrogen receptor. Therefore, [nat/Ga-68] 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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关键词
PET, Estrogen receptor, ER plus breast cancer, Bimodal imaging agent, Aggregate induced emission
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