Illuminating the Path to Target GPCR Structures and Functions

Abstract

G-protein-coupled receptors (GPCRs) are ubiquitous within eukaryotes, responsible for a wide array of physiological and pathological processes. Indeed, the fact that they are the most drugged target in the human genome is indicative of their importance. Despite the clear interest in GPCRs, most information regarding their activity has been so far obtained by analyzing the response from a ‘bulk medium’. As such, this perspective summarizes some of the common methods for this indirect observation. Nonetheless, by inspection of approaches applying super resolution imaging, we argue that imaging is perfectly situated to obtain more detailed structural and spatial information, assisting the development of new GPCR-targeted drugs and clinical strategies. The benefits of direct optical visualization of GPCRs are analyzed in the context of potential future directions in the field.