叶酸靶向抗肿瘤药物的研究进展

Recent advances in the folic acid-targeted anti-tumor drugs

叶酸受体在大多数肿瘤细胞表面高表达,而在正常细胞表面不表达或者非常少地表达。若叶酸能够携带肿瘤药物直接到达肿瘤病灶,那么通过叶酸受体介导的内吞作用将药物靶向递送到癌细胞,即可发挥与母药相当或者更高的疗效。这样肿瘤药物对正常细胞及组织的损害将大幅度降低,同时也可以提高药物的靶向性和药效。近几年来,叶酸靶向抗肿瘤药物的研究越来越受到科研工作者的关注,有的研究已经进入临床Ⅲ期阶段,例如叶酸-去乙酰长春碱单酰肼缀合物(EC145)。本文综述了最近几年来叶酸与抗肿瘤药物以化学键形成叶酸抗癌药物缀合物的研究现状。

Folate receptors highly express on the surface of most tumor cells,but don’t express or little express on the surface of normal cells.If folic acid carries the antitumor drug directly to the tumor lesion,then the drug could be targeted to the cancer cells through the endocytosis mediated by the folate receptor,and the therapeutic effect could be equivalent to or higher than that of the parent drug.In this w ay,the damage of the antitumor drugs to normal cells and tissues w ould be greatly reduced,and at the same time,the targeting and efficacy of the drugs could be improved.In recent years,folic acid-targeted antitumor drugs have draw n more and more attentions,even some conjugates have entered the clinical research stage,such as folic acid and desacetylvinblastine monohydrazide conjugate,w hich is under the phaseⅢclinical phase.This article review s the research progress of folic acid/anticancer drug conjugates formed via chemical bonds in recent years.