Selectively targeting cancer and infectious disease with fragment-based drug discovery

通过基于片段的药物发现选择性地针对癌症和传染病

• 批准号: DP140101495
• 负责人: Prof Sally-Ann Poulsen
• 金额: $ 27.24万
• 依托单位: Griffith University
• 依托单位国家: 澳大利亚
• 项目类别: Discovery Projects
• 财政年份: 2014
• 资助国家: 澳大利亚
• 起止时间: 2014-01-01 至 2017-12-31
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/DP140101495
• 关键词: Selectively; targeting; cancer; infectious; disease

Finding better compounds as starting points is one of the major challenges for drug discovery research. Fragments are small, weak binding molecules that can be upsized into drug leads with better properties when compared to starting with larger molecules. This project addresses two weaknesses of current fragment based drug discovery (FBDD) methods: first, the limitations associated with screening fragments; and second, the quality of commercial fragment libraries. This project anticipates that the findings will establish a commanding role for both mass spectrometry and three-dimensional fragments in advancing FBDD approaches. It also expects to identify fragments with favourable development prospects towards the next generation of therapeutics.

寻找更好的化合物作为起点是药物发现研究的主要挑战之一。片段是小的、弱的结合分子，与从更大的分子开始相比，它们可以被放大成具有更好性质的药物先导物。该项目解决了目前基于片段的药物发现（FBDD）方法的两个弱点：第一，与筛选片段相关的限制;第二，商业片段库的质量。该项目预计，研究结果将建立一个指挥官的作用，质谱和三维碎片在推进FBDD方法。它还期望鉴定出对下一代治疗具有有利发展前景的片段。