Glucose conjugation for the specific targeting and treatment of cancer.
Glucose conjugation for the specific targeting and treatment of cancer.
复制标题
DOI：
10.1039/c3sc22205e
复制
发表时间：
2013-06
期刊：
影响因子：
8.4
通讯作者：
Hergenrother PJ
中科院分区：
文献类型：
--
作者：
Calvaresi EC;Hergenrother PJ
不同来源的癌症表现出明显的葡萄糖亲和力和高有氧糖酵解率。随着对这种被称为华宝效应的功能失调代谢的了解的增加，人们对将其用于癌症治疗产生了兴趣。这种靶向的一个很有希望的策略是糖偶联，即将一种药物连接到葡萄糖或另一种糖上。该综述总结了糖偶联物的最突出的例子，在这些例子中，已知的细胞毒素或靶向抗癌治疗已经与葡萄糖(或另一种葡萄糖转运体底物糖)相连，以提高癌症的靶向性和选择性。在这些例子的基础上，本综述还为未来糖结合物的设计和机制评估提供了一系列指南。
Cancers of diverse origins exhibit marked glucose avidity and high rates of aerobic glycolysis. Increased understanding of this dysfunctional metabolism known as the Warburg effect has led to an interest in targeting it for cancer therapy. One promising strategy for such targeting is glycoconjugation, the linking of a drug to glucose or another sugar. This review summarizes the most salient examples of glycoconjugates, in which known cytotoxins or targeted anticancer therapeutics have been linked to glucose (or another glucose transporter substrate sugar) for improved cancer targeting and selectivity. Building on these examples, this review also provides a series of guidelines for the design and mechanistic evaluation of future glycoconjugates.