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- Title
Alpha-conotoxins as pharmacological probes of nicotinic acetylcholine receptors.
- Authors
AZAM, Layla; MCINTOSH, J. Michael
- Abstract
AbstractCysteine-rich peptides from the venom of cone snails (Conus) target a wide variety of different ion channels. One family of conopeptides, the α-conotoxins, specifically target different isoforms of nicotinic acetylcholine receptors (nAChRs) found both in the neuromuscular junction and central nervous system. This family is further divided into subfamilies based on the number of amino acids between cysteine residues. The exquisite subtype selectivity of certain α-conotoxins has been key to the characterization of native nAChR isoforms involved in modulation of neurotransmitter release, the pathophysiology of Parkinson's disease and nociception. Structure/function characterization of α-conotoxins has led to the development of analogs with improved potency and/or subtype selectivity. Cyclization of the backbone structure and addition of lipophilic moieties has led to improved stability and bioavailability of α-conotoxins, thus paving the way for orally available therapeutics. The recent advances in phylogeny, exogenomics and molecular modeling promises the discovery of an even greater number of α-conotoxins and analogs with improved selectivity for specific subtypes of nAChRs.Acta Pharmacologica Sinica (2009) 30: 771–783; doi: 10.1038/aps.2009.47; published online 18 May 2009
- Publication
Acta Pharmacologica Sinica, 2009, Vol 30, Issue 6, p771
- ISSN
1671-4083
- Publication type
Academic Journal
- DOI
10.1038/aps.2009.47