中文摘要：

叶酸是一种小分子量的维生素，其受体是一种糖蛋白，在肿瘤细胞膜表面高度表达；而在绝大多数正常组织中，几乎不表达。利用叶酸对叶酸受体的高度亲和性，可用于将药物与叶酸偶联，将药物靶向至肿瘤。对此，本文进行了综述。

英文摘要：

Folate, a low - molecular weight vitamin, when attacnea via γ, - carboxylate to any molecules retains its ability to specifically bind with its receptor： folate receptor （FR） without decreasing binding affinity. The FR is overexpressed on the surface of cancer cells in the case of epithelial malignancies, whereas it is expressed in very low levels in normal tissue. It quantitatively recycles between the cell surface and intracellular compartments internalizing receptor- bound folate/antifolate compounds and folate conjugates. Based on these certain distinctive advantages, folate targeting to tumor - specific drug delivery systems has become one of the most successful anticancer strategies in tumor therapy. In this article, brief and important mechanistic background of effective FR - targeted therapy is summarized and future prospects for folate targeted micromolecules and antifolates are also proposed.