叶酸受体在肿瘤靶向诊断和治疗中的应用

The role of folate receptors in the targeted diagnosis and treatment of carcinoma

叶酸受体(folate receptor,FR)是一种糖基磷脂酰肌醇(glycosylphosphatidylinositol,GPI)偶联蛋白。除个别组织外,叶酸受体在正常组织上表达水平很低,而在许多肿瘤细胞表面过表达。叶酸受体与叶酸及其衍生物有高度的亲和性,基于这种特性,可将显像剂、治疗药物等与叶酸偶联,靶向给予肿瘤细胞,从而应用于肿瘤的影像诊断如核医学显像、核磁共振显像、荧光显像和肿瘤治疗如化疗、同位素治疗、免疫治疗、反义核苷酸治疗及基因治疗中。

Folate receptor（FR） is a glycosylphosphatidylinositol（GPI） linked protein.Its expression is low in normal tissues except for some certain ones,but is high in a variety of human cancers.Based on the high affinity to the FR,imaging agents and drugs can be conjugated to folic acid and targeted delivered to tumor cells.FR-targeted agents can be applied to the imaging of tumors,such as nulear medicine imaging,MRI,fluorescence imaging as well as the treatment of tumors,such as chemotherapy,isotope therapy,immunotherapy,antisense oligodeoxynucleotide therapy and gene therapy.This review focused on the FR-based diagnosis and treatment of the cancers.