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

基于G蛋白偶联受体(GPCRs)的药物发现和开发可以通过有效利用聚合物脂质颗粒(PoLiPA)来简化。本项目的目的是研究可用于制备PoLiPA的新型聚合物，以制备纯化和稳定的G蛋白偶联受体GPCRs。在生产了含有GPCRs的PoLiPas之后，许多确定GPCRs结构、结合性质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)、低温电子显微镜(CRYO-EM)、微尺度热电泳法(MST)、质谱仪(MS)和动态光散射(DLS)。该项目的预测结果是对POLiPA的不同替代聚合物在3-4种不同技术上的有效性进行评估，这些技术在3种不同的GPCR的药物发现中很重要。这将使Polipas能够更有效地用于测试更广泛的GPCR。在不同的PoliPas上测试这些技术可能会提供GPCRs与其他蛋白质、脂类和分子相互作用的关键信息，这可能有助于开发新药。

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.