Modulation of T-type calcium channels by bioactive lipids - PubMed (original) (raw)

Review

. 2014 Apr;466(4):689-700.

doi: 10.1007/s00424-014-1467-5. Epub 2014 Feb 16.

Affiliations

Review

Modulation of T-type calcium channels by bioactive lipids

Jean Chemin et al. Pflugers Arch. 2014 Apr.

Abstract

T-type calcium channels (T-channels/CaV3) have unique biophysical properties allowing a calcium influx at resting membrane potential of most cells. T-channels are ubiquitously expressed in many tissues and contribute to low-threshold spikes and burst firing in central neurons as well as to pacemaker activities in cardiac cells. They also emerged as potential targets to treat cancer and hypertension. Regulation of these channels appears complex, and several studies have indicated that CaV3.1, CaV3.2, and CaV3.3 currents are directly inhibited by multiple endogenous lipids independently of membrane receptors or intracellular pathways. These bioactive lipids include arachidonic acid and ω3 poly-unsaturated fatty acids; the endocannabinoid anandamide and other N-acylethanolamides; the lipoamino-acids and lipo-neurotransmitters; the P450 epoxygenase metabolite 5,6-epoxyeicosatrienoic acid; as well as similar molecules with 18-22 carbons in the alkyl chain. In this review, we summarize evidence for direct effects of these signaling molecules, the molecular mechanisms underlying the current inhibition, and the involved chemical features. The impact of this modulation in physiology and pathophysiology is discussed with a special emphasis on pain aspects and vasodilation. Overall, these data clearly indicate that T-current inhibition is an important mechanism by which bioactive lipids mediate their physiological functions.

PubMed Disclaimer

Similar articles

Cited by

References

    1. J Lipid Res. 2003 Dec;44(12):2221-33 - PubMed
    1. Circ Res. 2005 Oct 28;97(9):908-15 - PubMed
    1. J Gen Physiol. 2004 Sep;124(3):225-38 - PubMed
    1. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1692-6 - PubMed
    1. Br J Pharmacol. 2011 Jun;163(3):484-95 - PubMed

Publication types

MeSH terms

Substances

LinkOut - more resources