Stabilising biased allosteric G protein-coupled receptor conformations

稳定偏向的变构 G 蛋白偶联受体构象

• 批准号: DP170104228
• 负责人: Dr Katie Leach
• 金额: $ 25.58万
• 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: 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/DP170104228
• 关键词: Stabilising; biased; allosteric; protein; coupled

This project aims to develop and identify molecules that can stabilise distinct calcium sensing receptor (CaSR) conformations. The CaSR is a G protein-coupled receptor (GPCR) vertebrates need to live. GPCRs are responsible for virtually all (patho)physiological processes. They are structurally very flexible, but this has hindered their structural determination. Developing and validating the proposed molecules should help future structural studies of an important GPCR. The project expects to enhance understanding of the structure and function of the CaSR and ultimately of the GPCR superfamily, which will ultimately lead to opportunities to discover new drugs.

该项目旨在开发和鉴定能够稳定不同钙敏感受体（CaSR）构象的分子。CaSR是脊椎动物生存所必需的G蛋白偶联受体（GPCR）。GPCR负责几乎所有（病理）生理过程。它们在结构上非常灵活，但这妨碍了它们在结构上的确定性。开发和验证所提出的分子应该有助于未来重要GPCR的结构研究。该项目预计将提高对CaSR的结构和功能的理解，并最终提高对GPCR超家族的理解，这将最终导致发现新药的机会。