Einstein Medical Center Philadelphia, Philadelphia, PA, USA.
Division of Kidney Diseases & Hypertension, Department of Medicine, School of Medicine & Health Sciences, The George Washington University, Washington, DC, USA.
Methods Mol Biol. 2021;2268:1-20. doi: 10.1007/978-1-0716-1221-7_1.
The understanding of how biological membranes are organized and how they function has constantly been evolving over the past decades. Instead of just serving as a medium in which specific proteins are located, certain parts of the lipid bilayer contribute to platforms that assemble signaling complexes by providing a microenvironment that facilitates effective protein-protein interactions. G protein-coupled receptors (GPCRs) and relevant signaling molecules, including the heterotrimeric G proteins, key enzymes such as kinases and phosphatases, trafficking proteins, and secondary messengers, preferentially partition to these highly organized cell membrane microdomains, called lipid rafts. Lipid rafts are essential for the trafficking and signaling of GPCRs. The study of GPCR biology in the context of lipid rafts involves the localization of the GPCR of interest in lipid rafts, at the basal state and upon receptor agonism, and the evaluation of the biological functions of the GPCR in appropriate cell lines. The lack of standardized methodologies to study lipid rafts, in general, and of the workings of GPCRs in lipid rafts, in particular, and the inescapable drawbacks of current methods have hampered the complete understanding of the underlying molecular mechanisms. Newer methodologies that allow the study of GPCRs in their native form are needed. The use of complementary approaches that produce mutually supportive results appears to be the best way for drawing conclusions with regard to the distribution and activity of GPCRs in lipid rafts.
在过去的几十年中,人们对生物膜的组织方式和功能的理解一直在不断发展。脂质双层的某些部分不仅作为特定蛋白质的定位介质,还通过提供有利于有效蛋白质-蛋白质相互作用的微环境,为组装信号复合物的平台做出贡献。G 蛋白偶联受体 (GPCR) 和相关信号分子,包括异三聚体 G 蛋白、关键酶如激酶和磷酸酶、运输蛋白和第二信使,优先分配到这些高度组织化的细胞膜微区,称为脂筏。脂筏对于 GPCR 的运输和信号转导至关重要。在脂筏的背景下研究 GPCR 生物学涉及到感兴趣的 GPCR 在基础状态和受体激动剂时在脂筏中的定位,以及在适当的细胞系中评估 GPCR 的生物学功能。缺乏标准化的方法来研究脂筏,一般来说,缺乏研究 GPCR 在脂筏中的作用的方法,特别是当前方法不可避免的缺点,阻碍了对潜在分子机制的全面理解。需要新的方法来研究其天然形式的 GPCR。使用互补方法来产生相互支持的结果,似乎是得出关于 GPCR 在脂筏中的分布和活性的结论的最佳方法。