Targeting the undruggable: epitope mapping using Phylomers peptides to modulate activity of Transcription Factors

靶向不可成药：使用 Phylomers 肽进行表位作图来调节转录因子的活性

• 批准号: LP140100798
• 负责人: A/Prof Yann Gambin
• 金额: $ 38.62万
• 依托单位: The University of New South Wales
• 依托单位国家: 澳大利亚
• 项目类别: Linkage Projects
• 财政年份: 2014
• 资助国家: 澳大利亚
• 起止时间: 2014-07-01 至 2018-01-14
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/LP140100798
• 关键词: Targeting; undruggable; epitope; mapping; using

This project aims at expanding the pool of drug targets, by extending drug screening to protein-protein interaction networks. This project aims to assemble a novel technical platform to detect binding between proteins, using a combination of cell-free protein expression, AlphaScreen and single-molecule fluorescence. This pipeline has great potential to accelerate the exploration of protein networks, and provides also a generic platform for drug screening on difficult targets. The project intends to screen Phylogica's libraries of peptides called Phylomers to discover tight binders to a Transcription Factor, Sox18. The objective of this project is to determine which Phylomers can disrupt specific interactions between Sox18 and its binding partners involved in lymphangiogenesis.

该项目旨在通过将药物筛选扩展到蛋白质-蛋白质相互作用网络来扩大药物靶点库。该项目旨在组装一个新的技术平台，使用无细胞蛋白表达，AlphaScreen和单分子荧光的组合来检测蛋白质之间的结合。这条管道具有加速蛋白质网络探索的巨大潜力，也为困难靶点的药物筛选提供了通用平台。该项目旨在筛选Phylogica的Phylomers肽库，以发现转录因子Sox 18的紧密结合物。该项目的目的是确定哪些Phylomers可以破坏Sox 18及其参与淋巴管生成的结合伙伴之间的特异性相互作用。