Molecular insight into allosteric modulation of G protein-coupled receptors

G 蛋白偶联受体变构调节的分子洞察

• 批准号: DE170100152
• 负责人: Dr David Thal
• 金额: $ 26.03万
• 依托单位: Monash University
• 依托单位国家: 澳大利亚
• 项目类别: Discovery Early Career Researcher Award
• 财政年份: 2017
• 资助国家: 澳大利亚
• 起止时间: 2017-01-01 至 2019-12-31
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/DE170100152
• 关键词: Molecular; insight; into; allosteric; modulation

The project aims to understand the molecular mechanisms underlying signal transduction and allosteric modulation of G protein-coupled receptors (GPCRs). Allosteric modulation of proteins is a fundamental process where two distinctly different binding sites are linked through a conformational change. This project will use structural biology, medicinal chemistry and analytical pharmacology to investigate how chemical probes modulate GPCRs at an atomic level, and understand the mechanisms underlying signal transduction. Project outcomes are intended to advance membrane protein crystallography and GPCR biology, and benefit the pharmaceutical industry.

该项目旨在了解G蛋白偶联受体（gpcr）信号转导和变构调节的分子机制。蛋白质的变构调节是两个截然不同的结合位点通过构象变化连接起来的基本过程。本项目将运用结构生物学、药物化学和分析药理学来研究化学探针如何在原子水平上调节gpcr，并了解信号转导的机制。项目成果旨在推进膜蛋白晶体学和GPCR生物学，并使制药行业受益。