αS-Conotoxin RVIIIA: A Structurally Unique Conotoxin That Broadly Targets Nicotinic Acetylcholine Receptors

Autor:	Elsie C. Jimenez, Russell W. Teichert, Baldomero M. Olivera
Rok vydání:	2005
Předmět:	Conus radiatus biology Pharmacology biology.organism_classification complex mixtures Biochemistry Nicotinic acetylcholine receptor Nicotinic agonist Ganglion type nicotinic receptor nervous system Conotoxin Alpha-4 beta-2 nicotinic receptor Nicotinic Antagonist Acetylcholine receptor
Zdroj:	Biochemistry. 44:7897-7902
ISSN:	1520-4995 0006-2960
DOI:	10.1021/bi047274+
Popis:	We report the purification and characterization of a new conotoxin from the venom of Conus radiatus. The peptide, αS-conotoxin RVIIIA (αS-RVIIIA), is biochemically unique with respect to its amino acid sequence, post-translational modification, and molecular targets. In comparison to other nicotinic antagonists from Conus venoms, αS-RVIIIA exhibits an unusually broad targeting specificity for nicotinic acetylcholine receptor (nAChR) subtypes, as assayed by electrophysiology. The toxin is paralytic to mice and fish, consistent with its nearly irreversible block of the neuromuscular nAChR. Similar to other antagonists of certain neuronal nAChRs, the toxin also elicits seizures in mice upon intracranial injection. The only previously characterized conotoxin from the S superfamily, σ-conotoxin GVIIIA, is a specific competitive antagonist of the 5-HT3 receptor; thus, αS-RVIIIA defines a novel family of nicotinic antagonists within the S superfamily. All previously characterized competitive conotoxin nAChR anta...
Databáze:	OpenAIRE
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