Alpha-conotoxins as pharmacological probes of nicotinic acetylcholine receptors

摘要: Cysteine-rich peptides from the venom of cone snails (Conus) target a wide variety different ion channels. One family conopeptides, α-conotoxins, specifically isoforms nicotinic acetylcholine receptors (nAChRs) found both in neuromuscular junction and central nervous system. This is further divided into subfamilies based on number amino acids between cysteine residues. The exquisite subtype selectivity certain α-conotoxins has been key to characterization native nAChR involved modulation neurotransmitter release, pathophysiology Parkinson's disease nociception. Structure/function led development analogs with improved potency and/or selectivity. Cyclization backbone structure addition lipophilic moieties stability bioavailability thus paving way for orally available therapeutics. recent advances phylogeny, exogenomics molecular modeling promises discovery an even greater specific subtypes nAChRs.