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Abstract：
G protein-coupled receptors (GPCRs) are a large family of integral membrane proteins which conduct a wide range of biological roles and represent significant drug targets. Most biophysical and structural studies of GPCRs have been conducted on detergent-solubilised receptors, and it is clear that detergents can have detrimental effects on GPCR function. Simultaneously, there is increasing appreciation of roles for specific lipids in modulation of GPCR function. Lipid nanoparticles such as nanodiscs and styrene maleic acid lipid particles (SMALPs) offer opportunities to study integral membrane proteins in lipid environments, in a form that is soluble and amenable to structural and biophysical experiments. Here, we review the application of lipid nanoparticle technologies to the study of GPCRs, assessing the relative merits and limitations of each system. We highlight how these technologies can provide superior platforms to detergents for structural and biophysical studies of GPCRs and inform on roles for protein-lipid interactions in GPCR function.
摘要：
G蛋白偶联受体（GPCRs）是一个完整的膜蛋白家族，具有广泛的生物学作用并代表重要的药物靶标。GPCRs的大多数生物物理和结构研究都是在去污剂溶解的受体上进行的，并且很明显去污剂可能对GPCR功能具有有害影响。同时,人们越来越认识到特定脂质在调节GPCR功能中的作用。脂质纳米颗粒，如纳米圆盘和苯乙烯马来酸脂质颗粒（SMALPs）提供了研究脂质环境中完整膜蛋白的机会，以可溶的形式，适合结构和生物物理实验。这里,本文综述了脂质纳米粒技术在GPCRs研究中的应用,评估每个系统的相对优点和局限性。我们强调这些技术如何为GPCR的结构和生物物理研究提供更好的去污剂平台，并告知蛋白质-脂质相互作用在GPCR功能中的作用。
