Toxins Targeting Voltage-Activated Ca2+ Channels and their Potential Biomedical Applications

Voltage-gated Ca2+ (Ca-V) channels are transmembrane proteins primarily formed by an ion-conducting alpha(1) subunit that can associate with auxiliary beta and alpha(2)delta subunits. Ca2+ entering the cell through these channels serves as a versatile second messenger of electrical signaling, initiating numerous different cellular processes ranging from gene expression to cell fertilization, neuronal transmission and cell death. Ca-V channels, as other ion channels, are targets for numerous ligands including naturally occurring peptide toxins. Some of these peptide toxins are invaluable tools for studying their structure and function and have potential therapeutic applications. Here, we present an overview of the current knowledge regarding the structure and function of Ca-V channels as well as their role in human disease, and highlight some of the growing applications of peptide toxins targeting Ca-V channels. Analysis and understanding of the molecular strategy used by these peptide toxins might allow the design of novel classes of therapeutic agents acting on specific targets with high selectivity and efficacy.