叶酸靶向的肿瘤治疗研究进展  

Current Research Progress of the Folate-Targeted Cancer Therapies

作　　者：杜长丽[1] 顾月清[1] 

机构地区：[1]中国药科大学生命科学与技术学院,江苏南京210009

出　　处：《药物生物技术》2012年第3期261-264,共4页Pharmaceutical Biotechnology

摘　　要：叶酸靶向的递药系统是一种新兴的治疗多种恶性肿瘤的方法。利用叶酸分子与肿瘤细胞表面叶酸受体的高亲和力,叶酸偶联的化合物能够将分子大小不同的复合物递送给病理细胞而不对正常组织造成伤害。目前,通过这种方法成功递送到叶酸受体高表达肿瘤细胞的复合物包括:蛋白毒素、化疗药物、免疫治疗剂、基因载体、反义寡核苷酸、小分子干扰RNA和纳米载体。该文综述了多种叶酸作为靶向配体治疗恶性肿瘤的方法。Folate targeted drug delivery has been emerged as an alternative therapy for the treatment of many cancers and inflamma- tory. Due to its small molecular size and high binding affinity to cell surface folate receptors （FR） ,which is a confirmed tumor-asso- ciated antigen that binds folate and folate-targeted drug conjugates with very high affinity and shuttles these bound molecules insides cells via an endocytic mechanism. Folate conjugates have the ability to deliver a variety of molecular complexes to folate receptor positive pathologic cells without causing harm to normal tissues. Complexes that have been successfully delivered to folate receptor expressing tumor ceils, to date, include protein toxins, chemotherapeutic agents, immune stimulants, vectors for gene therapy, antisense oligodeoxyribonucleotides （ODN）, small interfering RNAs （siRNA）, nanoparticles and so on. This review summarizes the applications of folic acid （FA） as a targeting ligand and highlights the various methods being developed for delivery of therapeutic agents to FR-expressing malignant ceils.

关 键 词：叶酸靶向 叶酸受体 癌症治疗 

分 类 号：R730.53[医药卫生—肿瘤]