Investigation into polymer lipid particles containing G-protein coupled receptors as a tool to drug discovery and drug detection

研究含有 G 蛋白偶联受体的聚合物脂质颗粒作为药物发现和药物检测的工具

• 批准号: 2433442
• 金额: --
• 依托单位: University of Birmingham
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2020
• 资助国家: 英国
• 起止时间: 2020 至 无数据
• 项目状态: 未结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2433442
• 关键词: Investigation; into; polymer; lipid; particles

Drug discovery and development based on G-protein coupled receptors (GPCRs) could be streamlined by efficient use of polymer lipid particles (PoLiPa). The aim of this project is to investigate new polymers that can be used to make PoLiPa in order to prepare purified and stable G-protein coupled receptors GPCRs. Many techniques important for determining GPCR structure, binding properties and biophysical characteristics become possible after producing PoLiPas containing GPCRs. This includes surface plasmon resonance (SPR); cryogenic electron microscopy (cryo-EM); microscale thermophoresis (MST); Mass Spectrometry (MS) and Dynamic Light scattering (DLS). The predicted outcome of the project is assessment of the effectiveness of different alternative polymers to PoLiPa on 3-4 different techniques important in drug discovery for 3 different GPCRs. This will allow more effective use of PoliPas for testing a wider range of GPCRs. Testing the techniques on different PoliPas may provide key information on GPCRs interact with other proteins, lipids and molecules which could be useful in developing a new drug.

高效利用聚合物脂质颗粒（PoLiPa）可以简化基于g蛋白偶联受体（gpcr）的药物发现和开发。该项目的目的是研究可用于制备PoLiPa的新聚合物，以制备纯化和稳定的g蛋白偶联受体gpcr。在生产含有GPCR的PoLiPas后，许多确定GPCR结构、结合特性和生物物理特性的重要技术成为可能。这包括表面等离子体共振（SPR）；低温电镜（cryo-EM）；微尺度热泳；质谱（MS）和动态光散射（DLS）。该项目的预测结果是评估不同的PoLiPa替代聚合物在3-4种不同技术上的有效性，这些技术在3种不同的gpcr药物发现中很重要。这将允许更有效地使用PoliPas来检测更广泛的gpcr。在不同的polipa上测试该技术可以提供GPCRs与其他蛋白质、脂质和分子相互作用的关键信息，这可能对开发新药有用。