Abstract
Highly selective N-type voltage-gated calcium (CaV) channel inhibitors from cone snail venom (the ω-conotoxins) have emerged as a new class of therapeutics for the treatment of chronic and neuropathic pain. Earlier in 2005, Prialt (Elan) or synthetic ω-conotoxin MVIIA, was the first ω-conotoxin to be approved by Food and Drug Administration for human use. This review compares the action of three ω-conotoxins, GVIA, MVIIA and CVID, describing their structure-activity relationships and potential as leads for the design of improved N-type therapeutics that are more useful in the treatment of chronic pain.
Highlights
There are approximately 500 different species of the genus Conus
This review describes the structure-activity relationship (SAR) and therapeutic potential of ω-conotoxin Ntype voltage-gated calcium channel (CaV) channel blockers form cone snails, the first of the conotoxin classes to be approved as a therapeutic
MVIIC has high sequence identity to MVIIA (Table 2), but quite different selectivity. Because of their high selectivity and affinity for neuronal CaV channels found in mammals, the ωconotoxins have become standard pharmacological reagents to investigate the role of CaV channels in neurotransmitter release [5, 8, 20,21,22,23]
Summary
There are approximately 500 different species of the genus Conus. Cone snails, found on the Great Barrier Reef in Australia and most other tropical waters around the world, are predatory marine gastropods they prey on fish, worms or molluscs [1]. Because of their high selectivity and affinity for neuronal CaV channels found in mammals, the ωconotoxins have become standard pharmacological reagents to investigate the role of CaV channels in neurotransmitter release [5, 8, 20,21,22,23] In addition to their use as research tools, animal studies have revealed that ω-conotoxins targeting N-type CaV channels have clinical potential in ischaemic brain injury [24, 25] and pain [26,27,28,29,30,31,32,33,34,35]. Six different α1 channel types named L-, T-, R-, P/Q- and N-type have been identified (Table 3)
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