Folate receptor (FR) is overexpressed on a large fraction of human cancers, while limited expression on normal cells. This makes it possible to utilize FR-targeted anticancer drugs which specially act on FR-positive tumor cells. This strategy also has improved the selectivity of drugs that may destroy the normal tissues in traditional chemotherapeutics. In addition, pro-drug has been widely accepted as an effective strategy in overcoming drug use barriers, enhancing chemical and metabolism stability, increasing the oral absorption degrees, enhancing the blood brain barrier permeability, improving the bioavailability, and reducing the adverse reactions of the application. In this review, the delivery mechanism of FR-targeted antitumor pro-drugs was introduced. Research and progress of this novel folate drug conjugates and their activities were also summarized.%叶酸受体(folate receptor,FR)在大部分人体肿瘤细胞表面过度表达,而在正常细胞表面则很少表达,甚至不表达.这就使得利用FR介导的抗肿瘤药物靶向作用于FR呈阳性的肿瘤细胞成为可能,从而减少传统抗癌药物对正常细胞的毒副作用.另外,前药在克服药物用药障碍、增强化学及代谢稳定性、增加口服或者局部给药的吸收度、增强血脑屏障渗透性、延长作用时间、提高生物利用度,以及减轻不良反应等应用中,已成为一种有效策略而被广为接受.本文主要对FR介导的抗肿瘤靶向前药的作用机制进行综述,并介绍近几年研究者设计并合成的叶酸修饰的靶向前药.
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