DNA interactions of polynuclear platinum. Mechanistic NMR studies probing the origin of the unique antitumour activity of BBR3464

多核铂的 DNA 相互作用。

• 批准号: DP0208117
• 负责人: Prof Susan Berners-Price
• 金额: $ 20.26万
• 依托单位: The University of Western Australia
• 依托单位国家: 澳大利亚
• 项目类别: Discovery Projects
• 财政年份: 2002
• 资助国家: 澳大利亚
• 起止时间: 2002-04-21 至 2005-12-31
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/DP0208117
• 关键词: DNA; interactions; polynuclear; platinum.; Mechanistic

BBR3464 is one of a class of structurally unique platinum anticancer drugs that is currently undergoing clinical trials. The anticancer activity most likely depends on binding to DNA, but the mechanism is quite different from that of the widely used drug, cisplatin. This project uses NMR spectroscopy to follow the processes involved in the initial binding of the drug to DNA and the subsequent reactions of the adducts formed. The results of this work will aid in the selection of back-up clinical candidates and in the design of drugs that target specific sequences of DNA for use in novel gene-based therapies.

BBR 3464是目前正在进行临床试验的一类结构独特的铂类抗癌药物之一。抗癌活性最可能取决于与DNA的结合，但其机制与广泛使用的药物顺铂的机制截然不同。 该项目使用NMR光谱法跟踪药物与DNA的初始结合过程以及形成的加合物的后续反应。 这项工作的结果将有助于选择备用临床候选药物，并设计针对特定DNA序列的药物，用于新的基因治疗。