Pharmacology and Structure-Function of Venom Peptide Inhibitors of N-Type (Cav2.2) Calcium Channels

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Voltage-Gated Calcium Channels


Venoms contain a complex mixture of mostly small peptides that are released from animals to facilitate prey capture and defensive strategies. An important class of neurotoxic venom peptides selectively inhibit specific types of voltage-gated ion channels, including N-type calcium channels (CaV2.2), that play a key role in the neurotransmission associated with pain pathways. In recognition of their importance as research tools and validated clinical potential, in this chapter, we highlight venom peptides that inhibit CaV2.2 (N-type calcium channels) and discuss their structure-activity relationships (SAR). Recent advances in our understanding of the mechanism of binding of CaV2.2-selective ω-conotoxins revealed from cryo-EM structures of the MVIIA-CaV2.2 complex allow the rational development of modified ω-conotoxins better able to treat severe pain conditions.

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