G-protein-coupled receptor modulation of voltage-gated ion channels is a common means of fine-tuning the response of channels to changes in membrane potential. Such modulation impacts physiological processes such as synaptic transmission, and hence therapeutic strategies often directly or indirectly target these pathways. As an exemplar of channel modulation, we examine strategies for investigating G-protein modulation of CaV2.2 or N-type voltage-gated Ca(2+) channels. We focus on biochemical and genetic tools for defining the molecular mechanisms underlying the various forms of CaV2.2 channel modulation initiated following ligand binding to G-protein-coupled receptors.
© 2016 Cold Spring Harbor Laboratory Press.