The structural basis of the G protein–coupled receptor and ion channel axis

Le résumé fourni par la source

Sensory neurons play an essential role in recognizing and responding to detrimental, irritating, and inflammatory stimuli from our surroundings, such as pain, itch, cough, and neurogenic inflammation. The transduction of these physiological signals is chiefly mediated by G protein-coupled receptors (GPCRs) and ion channels. The binding of ligands to GPCRs triggers a signaling cascade, recruiting G proteins or β-arrestins, which subsequently interact with ion channels (e.g., GIRK and TRP channels). This interaction leads to the sensitization and activation of these channels, initiating the neuron's protective mechanisms. This review delves into the complex interplay between GPCRs and ion channels that underpin these physiological processes, with a particular focus on the role of structural biology in enhancing our comprehension. Through unraveling the intricacies of the GPCR-ion channel axis, we aim to shed light on the sophisticated intermolecular dynamics within these pivotal membrane protein families, ultimately guiding the development of precise therapeutic interventions. • Sensory neurons transduce harmful stimuli via GPCRs/ion channels with ligand-GPCR binding triggers signaling cascade. • Structural study of GPCR-G protein-ion channel interactions provides understanding of the activation/sensitization. • Elucidating GPCR-channel axis structure enhances understanding on biomolecular complexes and targeted therapies.

Ce résumé expose les affirmations des auteurs. BNTIC ne l’interprète pas comme une validation indépendante des résultats.