Understanding multidrug resistance in cancer: identification of the substrate and inhibitor binding sites in P-glycoprotein

了解癌症的多药耐药性：P-糖蛋白中底物和抑制剂结合位点的鉴定

• 批准号: nhmrc : 1049685
• 负责人: A/Pr Richard Callaghan
• 金额: $ 18.96万
• 依托单位: The University of Queensland
• 依托单位国家: 澳大利亚
• 项目类别: Project Grants
• 财政年份: 2013
• 资助国家: 澳大利亚
• 起止时间: 2013-01-01 至 2016-12-31
• 项目状态: 已结题
• 来源: https://researchdata.edu.au/understanding-multidrug-resistance-p-glycoprotein/112103
• 关键词: Understanding; multidrug; resistance; cancer; identification

Cancers expressing the multidrug transporter P-glycoprotein (P-gp) are resistant to chemotherapy. The clinical impact of P-gp is so large that the National Cancer Institute (USA) “profiles” all anticancer drugs for transport by P-gp, primarily because the mechanism of drug binding and transport by P-gp is unknown. The aim of this proposal is to understand the molecular details of how drugs bind to and interact with P-gp, a major step in our understanding of P-gp mediated chemotherapy resistance.

表达多药转运蛋白P-糖蛋白（P-gp）的癌症对化疗具有抗性。P-gp的临床影响如此之大，以至于美国国家癌症研究所（National Cancer Institute，USA）对所有抗癌药物进行了P-gp转运的“概况”，主要是因为P-gp的药物结合和转运机制尚不清楚。本提案的目的是了解药物如何与P-gp结合和相互作用的分子细节，这是我们理解P-gp介导的化疗耐药性的重要一步。