Voltage-gated Ca2+ (CaV) channels are transmembrane proteins primarily formed by an
ion-conducting α 1 subunit that can associate with auxiliary β and α2δ 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. CaV 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 CaV channels as well as their role in human disease, and highlight some of the
growing applications of peptide toxins targeting CaV 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.
Keywords: Ca2+ channels, Cav channels, Conotoxins, Neuropathic pain, Ziconotide.
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