用于肿瘤靶向治疗的糖基前药研究进展

前药修饰是提高化疗药物肿瘤靶向性、降低药物毒副作用、提高抗肿瘤活性的有效策略。肿瘤细胞对糖的需求较正常细胞大幅提升，称之为Warburg效应。肿瘤细胞表面过表达葡萄糖转运蛋白或受体，且某些糖苷酶也在肿瘤组织高表达，因而糖基前药可实现抗肿瘤药物的靶向递送。近年来，多靶点、多功能的糖基前药发展迅速，设计更为巧妙、靶向性更强的糖基前药不断涌现，且糖基前药还被用于除肿瘤外其他多种疾病的靶向治疗。对近年来小分子糖基前药的研究进展进行综述和展望。

Research Progress in Glycoconjugate Prodrugs for Targeted Cancer Therapy

Prodrug modification is an effective strategy to improve chemotherapeutic drugs by increasing their tumor targetability,reducing side effects,and enhancing anticancer activity.The demand of tumor cells for glucose is much higher than that of normal cells,which is known as Warburg effect.Glucose transporters or receptors are over-expressed in many cancer cells,and the levels of some glycosidases are elevated in certain tumor tissues.As a result,glycoconjugate prodrugs are able to achieve targeted delivery of anticancer drugs.In recent years,with the accelerating development of multitarget and multifunctional glycoconjugate prodrugs,well-designed prodrugs with excellent tumor targetability are emerging,and the treatment scope of glycoconjugate prodrugs is broadening to many non-cancer diseases.In this paper,the research progress and prospect in small molecule glycoconjugate prodrugs is reviewed.