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糖基酶激活前药用于靶向癌症治疗。

Glycosidase activated prodrugs for targeted cancer therapy.

机构信息

School of Chemistry and Trinity Bioscience Institute, The University of Dublin, Trinity College Dublin, Dublin 2, Ireland.

SFI Synthesis and Solid State Pharmaceutical Centre (SSPC), Ireland.

出版信息

Chem Soc Rev. 2022 Nov 28;51(23):9694-9716. doi: 10.1039/d2cs00379a.

DOI:10.1039/d2cs00379a
PMID:36349720
Abstract

In this review glycosidase activated prodrugs that target cancer cells are discussed. Glycosylated prodrugs undergo enzymatic bioconversion, cleaving the prodrug to release the anticancer drug at the desired site of action, hence minimising the toxic side effects associated with many current anticancer drugs. In addition, the presence of the carbohydrate moiety increases the aqueous solubility of the drugs, allowing for a more effective treatment. In the past decade, significant advancements have been made in this field that have led to the development of many novel carbohydrate-based prodrugs - ranging from simple glycoconjugates to complex self-assemblies and materials, which are discussed in detail herein.

摘要

在这篇综述中,讨论了靶向癌细胞的糖苷酶激活前药。糖基化前药经历酶促生物转化,将前药裂解,在所需的作用部位释放抗癌药物,从而最大限度地减少许多现有抗癌药物相关的毒副作用。此外,碳水化合物部分的存在增加了药物的水溶解度,从而使治疗更有效。在过去的十年中,该领域取得了重大进展,导致了许多新型基于碳水化合物的前药的开发 - 从简单的糖缀合物到复杂的自组装和材料,本文对此进行了详细讨论。

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