甘肃医药2026，Vol.45Issue(7)：590-594,599,6.DOI:10.15975/j.cnki.1004-2725.2026.07.004
核素标记叶酸高分子聚合物肿瘤靶向探针研究进展
Research progress on radionuclide-labeled folate polymer tumor-targeted tracers
摘要
Abstract
Precision tumor diagnosis and targeted therapy represent the core development direction in precision medicine.The folate receptor(FR)is specifically overexpressed on the surface of epithelial-derived tumor cells,rendering it an ideal target for tumor-targeted theranostics.By employing high-affinity folic acid(FA)as a targeting ligand,conjugating it with functionalized polymeric carriers,and labeling them with radionuclides,tumor-targeting probes with strong affinity,favorable pharmacokinetics,and excellent imaging contrast can be con-structed.This article systematically elaborates on the molecular biological basis of folate targeting and the advantages of polymeric carriers,introduces the physicochemical properties and labeling chemistry of commonly used radionuclides(68Ga,18F,99mTc,64Cu,and 177Lu),analyzes the designand preparation of probe structures with different architectures and the modulation of in vivo pharmacokinetic behavior,with a fo-cus on the imaging sensitivity,specificity,and therapeutic efficacy in preclinical studies of FR-positive tumors.Additionally,it dissects the bottlenecks in clinical translation,encompassing issues such as high renal uptake,carrier biocompatibility,standardization of manufacturing processes,and biosafety.Finally,it provides perspectives on future directions,including intelligent probes,multimodal imaging,and theranos-tics,thereby offering a reference for the translational research of such probes.关键词
叶酸受体/高分子载体/放射性核素/靶向探针/诊疗一体化Key words
folate receptor/polymeric carriers/radionuclide/targeted probes/theranostics分类
医药卫生引用本文复制引用
达选祯,巨玉莲,曾贤伍,孙鹏,王天昊..核素标记叶酸高分子聚合物肿瘤靶向探针研究进展[J].甘肃医药,2026,45(7):590-594,599,6.基金项目
甘肃省自然科学基金项目(编号:20JR5RA158) （编号:20JR5RA158）
