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Toxins 2010, 2(6), 1471-1499; doi:10.3390/toxins2061471

Synthetic α-Conotoxin Mutants as Probes for Studying Nicotinic Acetylcholine Receptors and in the Development of Novel Drug Leads

Torrey Pines Institute for Molecular Studies, 11350 SW Village Pkwy, Port St Lucie, FL 34987, USA
Received: 1 April 2010 / Revised: 27 May 2010 / Accepted: 11 June 2010 / Published: 14 June 2010
(This article belongs to the Special Issue Toxins from Aquatic Organisms)
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Abstract

α-Conotoxins are peptide neurotoxins isolated from venomous marine cone snails that are potent and selective antagonists for different subtypes of nicotinic acetylcholine receptors (nAChRs). As such, they are valuable probes for dissecting the role that nAChRs play in nervous system function. In recent years, extensive insight into the binding mechanisms of α-conotoxins with nAChRs at the molecular level has aided in the design of synthetic analogs with improved pharmacological properties. This review examines the structure-activity relationship studies involving α-conotoxins as research tools for studying nAChRs in the central and peripheral nervous systems and their use towards the development of novel therapeutics.
Keywords: α-conotoxin; nicotinic acetylcholine receptor; acetylcholine binding protein; structure-activity relationship studies; mutational analysis α-conotoxin; nicotinic acetylcholine receptor; acetylcholine binding protein; structure-activity relationship studies; mutational analysis
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Armishaw, C.J. Synthetic α-Conotoxin Mutants as Probes for Studying Nicotinic Acetylcholine Receptors and in the Development of Novel Drug Leads. Toxins 2010, 2, 1471-1499.

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