• 放射性同位素应用技术 •

### 靶向叶酸受体的正电子分子探针研究进展

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
• 出版日期:2016-08-20 发布日期:2016-08-10

### 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

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.