Chemical Biology and Early Stages of Drug Discovery

化学生物学和药物发现的早期阶段

• 批准号: RGPIN-2015-05529
• 负责人: Tsantrizos, Youla
• 金额: $ 3.28万
• 依托单位: McGill University
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 财政年份: 2015
• 资助国家: 加拿大
• 起止时间: 2015-01-01 至 2016-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=590487
• 关键词: Chemical; Biology; Early; Stages; Drug

A key objective of our research program is the design and synthesis of molecular tools that can be used to probe the therapeutic value of biological targets. A related objective is the optimization of hit and lead compounds into pre-clinical candidates. These efforts mandate the development of efficient synthetic protocols that are amenable to modular, high throughput preparation of structurally diverse compound libraries. Fundamental to our research is the implementation of structural tools to guide our medicinal chemistry efforts. This proposal describes three of our projects, focusing on the human enzymes: 1. farnesyl pyrophosphate synthase (hFPPS), 2. geranylgeranyl pyrophosphate synthase (hGGPPS), and 3. the zinc metalloproteinase ZMPSTE24.

我们研究计划的一个关键目标是设计和合成可用于探测生物靶点治疗价值的分子工具。一个相关的目标是将命中化合物和先导化合物优化为临床前候选化合物。这些努力要求开发有效的合成方案，这些方案适合模块化、高通量制备结构多样的化合物库。我们研究的基础是实施结构工具来指导我们的药物化学工作。该提案描述了我们的三个项目，重点关注人类酶：1. 法尼基焦磷酸合酶 (hFPPS)、2. 香叶基香叶基焦磷酸合酶 (hGGPPS) 和 3. 锌金属蛋白酶 ZMPSTE24。