Structure determination of Fms and Kit kinases and their inhibtors for directed drug design

Fms 和 Kit 激酶及其抑制剂的结构测定，用于定向药物设计

• 批准号: nhmrc : 410505
• 负责人: Neal Williams
• 金额: $ 24.89万
• 依托单位: Monash University
• 依托单位国家: 澳大利亚
• 项目类别: Early Career Fellowships
• 财政年份: 2007
• 资助国家: 澳大利亚
• 起止时间: 2007-01-01 至 2009-12-31
• 项目状态: 已结题
• 来源: https://researchdata.edu.au/structure-determination-fms-drug-design/114874
• 关键词: Structure; determination; Fms; Kit; kinases

Tyrosine kinases are a large and important family of enzymes that play a fundamental role in the control and communication between cells. When damaged or uncontrolled, these enzymes can contribute to the development of diseases such as cancer and immune related disorders. This proposal aims to develop therapeutics targeted at the tyrosine kinases using a combination of the Structure Biology expertise at Monash University and the drug discovery platform technologies of Cytopia Pty Ltd. Promising drug candidates already identified by Cytopia will be analysed at their site of action using X-ray crystallography. This information will enable a rational process of modification and improvement of the candidate drugs. The development of a range of therapeutics for Phase I clinical trials will be of enormous benefit to Australia�s medical industry and pubic health.

酪氨酸激酶是一个庞大而重要的酶家族，在细胞之间的控制和通讯中发挥着重要作用。当受损或不受控制时，这些酶可能导致疾病的发展，如癌症和免疫相关疾病。该提案旨在开发针对酪氨酸激酶的治疗方法，结合莫纳什大学的结构生物学专业知识和Cytopia Pty Ltd的药物发现平台技术。Cytopia已经确定的有前途的候选药物将在其作用部位使用X射线晶体学进行分析。这些信息将使候选药物的修改和改进的合理过程成为可能。为I期临床试验开发一系列治疗药物将对澳大利亚的医疗行业和公共卫生产生巨大的好处。