Subtype-selective conopeptides targeted to nicotinic receptors:Concerted discovery and biomedical applications

Conus peptides that are selectively targeted to different molecular isoforms of nicotinic acetylcholine receptors (nAChRs) have been identified and characterized; several have recently been shown to have significant biomedical potential. An emerging strategy for the discovery from animal biodiversit...

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Bibliographic Details
Published in:Channels (Austin, Tex.) Tex.), 2008-03, Vol.2 (2), p.143-152
Main Authors: Olivera, Baldomero M, Quik, Maryka, Vincler, Michelle, McIntosh, J. Michael
Format: Article
Language:English
Subjects:
Animals
Binding
Biology
Bioscience
Calcium
Cancer
Cell
Conotoxins - pharmacology
Conus Snail
Cycle
Drug Delivery Systems
Drug Discovery - methods
Humans
Landes
Ligands
Organogenesis
Peptides - pharmacology
Proteins
Receptors, Nicotinic - drug effects
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Description
Summary:Conus peptides that are selectively targeted to different molecular isoforms of nicotinic acetylcholine receptors (nAChRs) have been identified and characterized; several have recently been shown to have significant biomedical potential. An emerging strategy for the discovery from animal biodiversity of subtype-specific ligands for ion channel families is described in this review. Characterization of the gene family encoding a set of related ligands is required for discovery using a molecular genetics approach; when discovery is guided by a knowledge of the phylogeny of the biodiverse animal lineage being used as a source of ligands, a rational, efficient scan of the library of putative ligands becomes feasible. Together, these constitute an approach to uncover subtype-specific ligands, called "concerted discovery"; this was applied to the α-conotoxins, a family of Conus peptides generally targeted to nAChRs.
ISSN:1933-6950
1933-6969
DOI:10.4161/chan.2.2.6276