Regulation of CaV2 calcium channels by G protein coupled receptors

► CaV2 channels play pivotal roles in neurotransmitter and hormone release. ► G protein coupled receptors orchestrate precise control of CaV2 channels. ► Voltage-dependent inhibition is mediated by direct binding of Gβγ to the channels. ► Voltage-independent inhibition is mediated by several other distinct pathways. ► Current understanding of these important mechanisms is provided in this review.