Design, synthesis, and evaluation of heparan sulfate mimicking glycopolymers for inhibiting heparanase activity

被引：37

作者：

Loka, Ravi S. ^{[1
]}

Yu, Fei ^{[1
]}

Sletten, Eric T. ^{[1
]}

Nguyen, Hien M. ^{[1
]}

机构：

[1] Univ Iowa, Dept Chem, Iowa City, IA 52242 USA

来源：

CHEMICAL COMMUNICATIONS | 2017年 / 53卷 / 65期

关键词：

TUMOR-GROWTH; ANGIOGENESIS; EXPRESSION; BINDING; AGGLUTINATION; PROTEOGLYCANS; METASTASIS; MIMETICS; RELEASE; CANCER;

D O I：

10.1039/c7cc04156j

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Heparanase is an enzyme which cleaves heparan sulfate (HS) polysaccharides of the extracellular matrix. It is a regulator of tumor behavior, plays a key role in kidney related diseases and autoimmune diabetes. We report herein the use of computational studies to extract the natural HS-heparanase interactions as a template for the design of HS mimicking glycopolymers. Upon evaluation, a glycopolymer with 12 repeating units was determined to be the most potent inhibitor and to have tight-binding characteristics. This glycopolymer also lacks anticoagulant activity.

引用

页码：9163 / 9166

页数：4

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