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α-Conotoxin GI Triazole-Peptidomimetics: Potent and Stable Blockers of a Human Acetylcholine Receptor

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By Laura McDougall, Rachel Whiting, Astrid Knuhtsen, Fergus S McWhinnie
| Royal Society of Chemistry Verified
The potency and selectivity of conotoxin peptides for neuropathic receptors has made them attractive lead compounds in the development of new therapeutics. Specifically, α-conotoxin GI has been shown to be an unparalleled antagonist of the nicotinic acetylcholine receptor (nAChR). However, as with other peptidic leads, poor protease resistance and the redox instability of the conotoxin scaffold limits bioactivity.
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