Capturing the dynamics of G-protein-coupled receptors (GPCRs) as they transduce extracellular signals into key physiological processes remains one of the most challenging research areas over the last two decades. Meanwhile, more recent attention has turned to the action of solute carriers (SLCs) that comprise both facilitative transporters and secondary active transporters. Because GPCRs and SLCs play critical roles in health and disease, and thereby serve as major targets for drug discovery, much effort has focused on capturing their various conformational states using conventional structural biology techniques. Here, we consider roles that mass spectrometry-based approaches play, particularly with respect to uncovering the impact of phosphorylation, defining ligands, and revealing the action of lipids in modulating interactions, transport, and conformational dynamics.

捕获 G 蛋白偶联受体 (GPCR) 将细胞外信号转导为关键生理过程时的动态仍然是过去二十年中最具挑战性的研究领域之一。与此同时，最近的注意力转向了溶质载体（SLC）的作用，其中包括易化转运蛋白和次级主动转运蛋白。由于 GPCR 和 SLC 在健康和疾病中发挥着关键作用，因此成为药物发现的主要靶标，因此许多努力集中在使用传统结构生物学技术捕获它们的各种构象状态。在这里，我们考虑基于质谱的方法所发挥的作用，特别是在揭示磷酸化的影响、定义配体以及揭示脂质在调节相互作用、运输和构象动力学中的作用方面。