Abstract
RGK proteins belong to the Ras superfamily of monomeric G-proteins, and currently include four members - Rad, Rem, Rem2, and Gem/Kir. RGK proteins are broadly expressed, and are the most potent known intracellular inhibitors of high-voltage-activated Ca²⁺ (Ca(V)1 and Ca(V)2) channels. Here, we review and discuss the evidence in the literature regarding the functional mechanisms, structural determinants, physiological role, and potential practical applications of RGK-mediated inhibition of Ca(V)1/Ca(V)2 channels. This article is part of a Special Issue entitled: Calcium channels.