Calvaresi Emilia C, Hergenrother Paul J
Department of Biochemistry, University of Illinois, Urbana, IL 61801.
Chem Sci. 2013 Jun;4(6):2319-2333. doi: 10.1039/C3SC22205E.
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.
起源各异的癌症表现出显著的葡萄糖亲和力和高有氧糖酵解速率。对这种被称为瓦伯格效应的功能失调代谢的深入了解，引发了人们将其作为癌症治疗靶点的兴趣。这种靶向治疗的一个有前景的策略是糖缀合，即将药物与葡萄糖或另一种糖类连接。本综述总结了糖缀合物的最显著例子，其中已知的细胞毒素或靶向抗癌治疗药物已与葡萄糖（或另一种葡萄糖转运体底物糖）连接，以提高癌症靶向性和选择性。基于这些例子，本综述还为未来糖缀合物的设计和机制评估提供了一系列指导方针。
