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Mar. Drugs 2014, 12(5), 2970-3004; doi:10.3390/md12052970
Review

Conotoxins Targeting Nicotinic Acetylcholine Receptors: An Overview

,
,
 and
*
Toxicology and Pharmacology, KU Leuven (University of Leuven), O&N2 P.O.Box 922, Herestraat 49, 3000 Leuven, Belgium
* Author to whom correspondence should be addressed.
Received: 31 March 2014 / Revised: 24 April 2014 / Accepted: 28 April 2014 / Published: 22 May 2014
(This article belongs to the Special Issue Bioactive Compounds from Marine Invertebrates)
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Abstract

Marine snails of the genus Conus are a large family of predatory gastropods with an unparalleled molecular diversity of pharmacologically active compounds in their venom. Cone snail venom comprises of a rich and diverse cocktail of peptide toxins which act on a wide variety of ion channels such as voltage-gated sodium- (NaV), potassium- (KV), and calcium- (CaV) channels as well as nicotinic acetylcholine receptors (nAChRs) which are classified as ligand-gated ion channels. The mode of action of several conotoxins has been the subject of investigation, while for many others this remains unknown. This review aims to give an overview of the knowledge we have today on the molecular pharmacology of conotoxins specifically interacting with nAChRs along with the structure–function relationship data.
Keywords: nicotinic acetylcholine receptor; cone snail toxins; α-conotoxins; mode of action; working mechanism; acetylcholine binding protein; crystallography; docking model nicotinic acetylcholine receptor; cone snail toxins; α-conotoxins; mode of action; working mechanism; acetylcholine binding protein; crystallography; docking model
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Lebbe, E.K.M.; Peigneur, S.; Wijesekara, I.; Tytgat, J. Conotoxins Targeting Nicotinic Acetylcholine Receptors: An Overview. Mar. Drugs 2014, 12, 2970-3004.

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