Exploring functional consequences of GPCR oligomerization requires a different lens.

摘要: As the largest family of cell surface receptors, G protein-coupled receptors (GPCRs) represent an important strategic class therapeutic targets. Attaining a clearer perspective how such signaling complexes set molecular events in motion could have significant impact on our understanding and treatment human diseases. such, many experimental approaches out to better understand networks associated with individual architectures their relationship outcomes. However, designing vitro assays aimed at addressing downstream single GPCRs must also take into account propensity form homo- heterooligomeric complexes. In context GPCR oligomers, physical interactions partner protein can number potential consequences, which we will explore this review. We discuss methods used identify putative dimer partners as well various techniques study functional consequences complex formation. Since full significance physiological relevance oligomers remains incompletely understood, owing part technical limitations, new tools elucidate mechanisms underlying allosteric co-regulation occurring between two are required. Accordingly, using example FP/AT1R heterodimer, FlAsH-BRET approach simple tool reveal information is transmitted via conformational rearrangements within means deorphanize receptors.