PT  - JOURNAL ARTICLE
AU  - H. William Tedford
AU  - Gerald W. Zamponi
TI  - Direct G Protein Modulation of Ca<sub>v</sub>2 Calcium Channels
AID  - 10.1124/pr.58.4.11
DP  - 2006 Dec 01
TA  - Pharmacological Reviews
PG  - 837--862
VI  - 58
IP  - 4
4099  - http://pharmrev.aspetjournals.org/content/58/4/837.short
4100  - http://pharmrev.aspetjournals.org/content/58/4/837.full
SO  - Pharmacol Rev2006 Dec 01; 58
AB  - The regulation of presynaptic, voltage-gated calcium channels by activation of heptahelical G protein-coupled receptors exerts a crucial influence on presynaptic calcium entry and hence on neurotransmitter release. Receptor activation subjects presynaptic N- and P/Q-type calcium channels to a rapid, membrane-delimited inhibition—mediated by direct, voltage-dependent interactions between G protein βγ subunits and the channels—and to a slower, voltage-independent modulation involving soluble second messenger molecules. In turn, the direct inhibition of the channels is regulated as a function of many factors, including channel subtype, ancillary calcium channel subunits, and the types of G proteins and G protein regulatory factors involved. Twenty-five years after this mode of physiological regulation was first described, we review the investigations that have led to our current understanding of its molecular mechanisms.