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Toxins
06, 2010;2 (6): 1471-99.

Synthetic α-conotoxin mutants as probes for studying nicotinic acetylcholine receptors and in the development of novel drug leads.

Christopher J Armishaw
Author Information
  1. Christopher J Armishaw: Torrey Pines Institute for Molecular Studies, 11350 SW Village Pkwy, Port St Lucie, FL 34987, USA. carmishaw@tpims.org
PMID: 22069647 DOI: 10.3390/toxins2061471

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

acetylcholine binding protein mutational analysis nicotinic acetylcholine receptor structure-activity relationship studies α-conotoxin

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MeSH Term

Animals
Conotoxins
Humans
Mutation
Neurotoxins
Nicotinic Antagonists
Protein Conformation
Receptors, Nicotinic
Structure-Activity Relationship

Chemicals

Conotoxins
Neurotoxins
Nicotinic Antagonists
Receptors, Nicotinic
Journal Article Review

Word Cloud

Created with Highcharts 10.0.0acetylcholinenAChRsnicotinicreceptorsprobesnervousbindingα-conotoxinsstructure-activityrelationshipstudiesstudyingdevelopmentnovelα-conotoxinα-ConotoxinspeptideneurotoxinsisolatedvenomousmarineconesnailspotentselectiveantagonistsdifferentsubtypesvaluabledissectingroleplaysystemfunctionrecentyearsextensiveinsightmechanismsmolecularlevelaideddesignsyntheticanalogsimprovedpharmacologicalpropertiesreviewexaminesinvolvingresearchtoolscentralperipheralsystemsusetowardstherapeuticsSyntheticmutantsdrugleadsproteinmutationalanalysisreceptor

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