Kulkarni Harshad R, Singh Aviral, Langbein Thomas, Schuchardt Christiane, Mueller Dirk, Zhang Jingjing, Lehmann Coline, Baum Richard P
1 Theranostics Center for Molecular Radiotherapy and Molecular Imaging, Zentralklinik Bad Berka , Bad Berka , Germany.
Br J Radiol. 2018 Nov;91(1091):20180308. doi: 10.1259/bjr.20180308. Epub 2018 Jun 1.
Alterations at the molecular level are a hallmark of cancer. Prostate cancer is associated with the overexpression of prostate-specific membrane antigen (PSMA) in a majority of cases, predominantly in advanced tumors, increasing with the grade or Gleason's score. PSMA can be selectively targeted using radiolabeled PSMA ligands. These small molecules binding the PSMA can be radiolabeled with γ-emitters like Tc and In or positron emitters like Ga and F for diagnosis as well as with their theranostic pairs such as Lu (β-emitter) or Ac (α-emitter) for therapy. This review summarizes the theranostic role of PSMA ligands for molecular imaging and targeted molecular radiotherapy, moving towards precision oncology.
分子水平的改变是癌症的一个标志。在大多数情况下，前列腺癌与前列腺特异性膜抗原（PSMA）的过表达有关，主要发生在晚期肿瘤中，并随着肿瘤分级或 Gleason 评分的增加而升高。PSMA 可以使用放射性标记的 PSMA 配体进行选择性靶向。这些与 PSMA 结合的小分子可以用 γ 发射体如 Tc 和 In 或正电子发射体如 Ga 和 F 进行放射性标记用于诊断，也可以用它们的治疗诊断配对物如 Lu（β 发射体）或 Ac（α 发射体）进行放射性标记用于治疗。本综述总结了 PSMA 配体在分子成像和靶向分子放疗中的治疗诊断作用，朝着精准肿瘤学迈进。
