Development of a new high throughput screen for drug binding to hERG K+ channels

开发新的高通量筛选药物与 hERG K 通道的结合

• 批准号: nhmrc : 1000587
• 负责人: Dr Mark Treherne
• 金额: $ 23.43万
• 依托单位: Victor Chang Cardiac Research Institute
• 依托单位国家: 澳大利亚
• 项目类别: NHMRC Development Grants
• 财政年份: 2010
• 资助国家: 澳大利亚
• 起止时间: 2010-01-01 至 2012-12-31
• 项目状态: 已结题
• 来源: https://researchdata.edu.au/development-new-high-k-channels/97728
• 关键词: Development; new; throughput; screen; drug

Inadvertent drug block of hERG, a potassium channel in the heart, can cause cardiac arrhythmias and sudden cardiac death. Screening for hERG toxicity has become a major hurdle for development of new drugs. We will use a mutant hERG protein that has enhanced drug binding to develop a high throughput test for hERG toxicity. Identification of dangerous drugs early in the drug discovery process will save the pharmaceutical industry millions of dollars in the costs of brining new drugs to market.

无意中药物阻断 hERG（心脏中的钾通道）可导致心律失常和心源性猝死。 hERG 毒性筛选已成为新药开发的主要障碍。我们将使用增强药物结合的突变 hERG 蛋白来开发 hERG 毒性的高通量测试。在药物发现过程的早期识别危险药物将为制药行业节省数百万美元的新药上市成本。