Conotoxins targeting nicotinic acetylcholine receptors: an overview

• Published in: Marine Drugs Vol. 12; no. 5; pp. 2970 - 3004
• Main Authors: Lebbe, Eline K M, Peigneur, Steve, Wijesekara, Isuru, Tytgat, Jan
• Format: Journal Article Book Review
• Language: English
• Published: Switzerland MDPI AG 22.05.2014; MDPI
• Subjects: acetylcholine binding protein; Amino Acid Sequence; Animals; Calcium Channel Blockers - pharmacology; cone snail toxins; Conotoxins - chemistry; Conotoxins - genetics; Conotoxins - pharmacology; Conus; Conus Snail - physiology; crystallography; docking model; Gastropoda; Humans; Marine; mode of action; Models, Molecular; Molecular Conformation; Molecular Sequence Data; nicotinic acetylcholine receptor; Receptors, Nicotinic - drug effects; Review; Structure-Activity Relationship; working mechanism; α-conotoxins
• ISSN: 1660-3397; 1660-3397
• DOI: 10.3390/md12052970

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.