JOURNAL OF ISOTOPES

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PET Molecular Probes Targeting Folate Receptor

YIN Ji-lin1;WANG Cheng2;WANG Xin-lu1   

  1. 1.PET-CT Center, Guangzhou General Hospital of Guangzhou Military Command, Guangzhou 510010, China;2.Department of Nuclear Medicine, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China
  • Online:2016-08-20 Published:2016-08-10

靶向叶酸受体的正电子分子探针研究进展

尹吉林1;王成2;王欣璐1   

  1. 1.广州军区广州总医院 PET/CT中心,广东 广州510010;2.上海交通大学 医学院附属仁济医院 核医学科,上海200127

Abstract:

Folic acid can combine specifically with folate receptors (FRs) which are overexpressed on the epithelial cells of the tumor. The FRs are confirmed to be the tumor-associated antigens that bind folate and folate conjugates with very high affinity and shuttle these bound molecules inside cells via an endocytic mechanism.The FR-α is a target of critical value for nuclear imaging through using folate-based radiotracers as it is expressed on several tumor types. Moreover, employment of folate radiopharmaceuticals for imaging of inflammatory diseases by targeting at FR-β on activated macrophages holds promise as a further field of application. Based on these, more and more researches focus on folate conjugates labeled with radionuclides for nuclear medicine imaging (including single photon emission computed tomography (SPECT) and positron emission tomography (PET). These folate molecular probes are applied not only in cancer imaging but also in inflammation imaging. Hence, folate-based imaging agents may be useful for selection of patients who could profit from such new therapy concepts and for monitoring response to a particular treatment. This review was focused on the preparation and preclinical biological evaluation of the molecular probes which were labeled by positron nuclides (18F, 124I, 68Ga, 44Sc, 152Tb), and the clinical application of these molecular probes were discussed.

Key words: folate receptor, molecular probe, positron emission tomography

摘要:

叶酸能与多种肿瘤细胞膜表面的叶酸受体(FR)特异性结合,通过FR介导的内吞作用进入细胞,为放射性核素选择性载带提供良好的途径。基于受体和配体间的高度亲和性,可将多种放射性核素与叶酸分子及其衍生物偶联,制备核医学显像探针。本文主要对非金属正电子核素(18F、124I)和金属正电子核素(68Ga、44Sc、152Tb)标记的叶酸及其衍生物PET显像探针与炎症PET显像探针进行综述,并展望其临床前景。

关键词: 叶酸受体, 分子探针, 正电子发射计算机断层扫描