正电子发射/三嗪花菁荧光对比剂在前列腺癌影像引导管理中的应用。
F-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management.
机构信息
Department of Radiology, Molecular Imaging Innovations Institute , Weill Cornell Medicine , New York , New York 10065 , United States.
Department of Radiology , Memorial Sloan Kettering Cancer Center , New York , New York 10065 , United States.
出版信息
J Med Chem. 2018 May 10;61(9):4256-4262. doi: 10.1021/acs.jmedchem.8b00240. Epub 2018 Apr 20.
Abstract
[F]-4, an anionic GCPII/PSMA inhibitor for image-guided intervention in prostate cancer, is described. [F]-4 is radiolabeled with a radiochemical yield that is ≥27% and a molar activity of 190 ± 50 mCi/μmol in a <1 h, one-step, aqueous isotopic exchange reaction. [F]-4 allows PSMA expression to be imaged by fluorescence (FL) and [F]-PET. PC3-PIP (PSMA-positive, EC = 6.74 ± 1.33 nM) cancers are specifically delineated in mice that bear 3 million (18 mg) PC3-PIP and PC3 (control, PSMA-negative) cells. Colocalization of [F]-4 PET, fluorescence, scintillated biodistribution, and PSMA expression are observed.
摘要
描述了一种阴离子 GCPII/PSMA 抑制剂 [F]-4，用于前列腺癌的影像引导介入。[F]-4 通过放射性化学收率≥27%和摩尔活度 190±50mCi/μmol 在 1 小时内的一步水相同位素交换反应进行放射性标记。[F]-4 允许通过荧光 (FL) 和 [F]-PET 成像 PSMA 表达。在携带 300 万 (18mg) PC3-PIP 和 PC3(对照，PSMA 阴性)细胞的小鼠中，特异性描绘出 PSMA 阳性、EC=6.74±1.33nM 的 PC3-PIP 癌症。观察到 [F]-4 PET、荧光、闪烁生物分布和 PSMA 表达的共定位。
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