Synthetic α-conotoxin Mutants As Probes for Studying Nicotinic Acetylcholine Receptors and in the Development of Novel Drug Leads

Overview

Journal Toxins (Basel)

Publisher MDPI

Specialty Toxicology

Date 2011 Nov 10

PMID 22069647

Citations 18

Authors

Christopher J Armishaw

Affiliations

Soon will be listed here.

Abstract

α-Conotoxins are peptide neurotoxins isolated from venomous marine cone snails that are potent and selective antagonists for different subtypes of nicotinic acetylcholine receptors (nAChRs). As such, they are valuable probes for dissecting the role that nAChRs play in nervous system function. In recent years, extensive insight into the binding mechanisms of α-conotoxins with nAChRs at the molecular level has aided in the design of synthetic analogs with improved pharmacological properties. This review examines the structure-activity relationship studies involving α-conotoxins as research tools for studying nAChRs in the central and peripheral nervous systems and their use towards the development of novel therapeutics.

Citing Articles

Chemical Synthesis and Insecticidal Activity Research Based on α-Conotoxins.

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Potency- and Selectivity-Enhancing Mutations of Conotoxins for Nicotinic Acetylcholine Receptors Can Be Predicted Using Accurate Free-Energy Calculations.

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Interactions of the α3β2 Nicotinic Acetylcholine Receptor Interfaces with α-Conotoxin LsIA and its Carboxylated C-terminus Analogue: Molecular Dynamics Simulations.

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Sudewi A, Susilawathi N, Mahardika B, Mahendra A, Pharmawati M, Phuong M ACS Omega. 2019; 4(21):19483-19490.

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