Metalloglycomics: A New Approach to Glycan Targeting

Metalloglycomics：一种定位聚糖的新方法

• 批准号: DP150100308
• 负责人: Prof Susan Berners-Price
• 金额: $ 32.66万
• 依托单位: Griffith University
• 依托单位国家: 澳大利亚
• 项目类别: Discovery Projects
• 财政年份: 2015
• 资助国家: 澳大利亚
• 起止时间: 2015-01-01 至 2019-06-30
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/DP150100308
• 关键词: Metalloglycomics; New; Approach; Glycan; Targeting

Proteoglycans and their associated enzymes are significant emerging drug targets of high biological relevance. This project explores a new approach to drug design based on high affinity binding to carbohydrates by polynuclear platinum compounds. Nuclear magnetic resonance spectroscopy studies will be used to delineate structure-activity relationships and the novel technique nano-scale secondary ion mass spectrometry will be developed to explore the mechanism of cellular uptake and sub-cellular distribution. The results will provide mechanistic understanding underpinning the future development of dual-action platinum anticancer drugs with both DNA binding and anti-angiogenic activity.

蛋白聚糖及其相关酶是具有高度生物相关性的重要新兴药物靶标。该项目探索了一种基于多核铂化合物与碳水化合物的高亲和力结合的药物设计新方法。核磁共振波谱研究将用于描述构效关系，纳米尺度二次离子质谱将用于探索细胞摄取和亚细胞分布的机制。这些结果将为未来开发具有DNA结合和抗血管生成活性的双作用铂类抗癌药物提供机制上的理解。