Deyi Zhao,Yongqi Han,Yamei Chen,Zhenyang He,Qian Xia,Ding-Kun Ji,Weihong Tan
Triple-negative breast cancer (TNBC) is one of the most malignant cancer types, characterized by a lack of efficient diagnostic and treatment methods in clinical practice. The development of effective targeted diagnosis and treatment for TNBC has become an important research focus. Here, we report the first proof-of-concept evidence of a glycoaptamer dual-target radionuclide probe (GDRP) for positron emission tomography/computed tomography (PET/CT) imaging of TNBC. The GDRP was created through precise molecular engineering of the aptamer AS1411, combined with three mannose ligands. The GDRP exhibited significantly increased serum stability and a high affinity for TNBC cells through a dual targeting mode. The advantages of our developed GDRP were further demonstrated by its excellent in vivo PET/CT dynamic imaging performance, featuring a long imaging window and high spatiotemporal resolution. This flexible method allows for the preparation of glycosylated functional nucleic acid molecular probes with high serum stability and tumor specificity. We anticipate that this PET/CT molecular probe will expand the development of glycoaptamer-based radioactive drugs and provides molecular tools for the clinical diagnosis of TNBC.
Prostate-specific membrane antigen (PSMA) is a prostate cancer target that plays a crucial role in prostate cancer diagnosis and therapy. Herein, a novel dual-targeted imaging probe, [68Ga]Ga-FAPI-PSMA, was prepared by radiolabeling conjugated DOTA-FAPI-PSMA with the short half-life radionuclide gallium-68 (68Ga), which is dedicated to prostate cancer diagnostic imaging. In vitro, [68Ga]Ga-FAPI-PSMA had higher affinity for the PSMA and FAP high-expressing cell lines 22Rv1 and U87 MG with IC50 values of 4.73 and 2.10 nM, respectively, than in the corresponding negative expression cell lines PC3 and A549, and significant differences in cell uptake were also observed. In vivo, [68Ga]Ga-FAPI-PSMA was rapidly cleared from the body, and the estimated radiation dose was relatively low compared with several other FAPI probes. In 22Rv1 and U87 MG tumor xenografts, [68Ga]Ga-FAPI-PSMA rapidly accumulated in tumors after administration, and the best images can be obtained at 1 h postinjection. In conclusion, the dual-targeted probe [68Ga]Ga-FAPI-PSMA was successfully prepared for in vivo prostate cancer PET/CT imaging.
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