Allosteric and Bitopic Ligands Acting at G Protein-Coupled Receptors

作用于 G 蛋白偶联受体的变构和双位配体

• 批准号: DP160101970
• 负责人: Prof Peter Scammells
• 金额: $ 46.82万
• 依托单位: Monash University
• 依托单位国家: 澳大利亚
• 项目类别: Discovery Projects
• 财政年份: 2016
• 资助国家: 澳大利亚
• 起止时间: 2016-01-01 至 2019-12-31
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/DP160101970
• 关键词: Allosteric; Bitopic; Ligands; Acting; Protein

This project seeks to gain a more detailed understanding of the mechanisms of the function of G protein-coupled receptors (GPCRs) using novel chemical tools. GPCRs are the largest group of cell surface signalling proteins and are responsible for the regulation of numerous vital physiological functions. They are the target of over 30 per cent of currently used pharmaceuticals. Despite their importance, much remains to be learned about the regulation of GPCRs by small molecules. This project aims to address this gap by focusing on novel regions on these proteins, termed allosteric sites, to explore novel modes of GPCR regulation which may offer the potential of identifying pathway selective agents.

该项目旨在使用新的化学工具更详细地了解G蛋白偶联受体（GPCR）的功能机制。GPCR是最大的细胞表面信号蛋白组，负责调节许多重要的生理功能。它们是目前使用的30%以上药品的目标。尽管它们很重要，但关于小分子对GPCR的调控仍有很多东西需要了解。该项目旨在通过关注这些蛋白质上的新区域（称为变构位点）来解决这一差距，以探索GPCR调控的新模式，这可能提供识别途径选择性试剂的潜力。