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Scorpion Toxins Specific for Potassium (K+) Channels: A Historical Overview of Peptide Bioengineering

Department of Molecular Biosciences and Bioengineering, College of Tropical Agriculture and Human Resources, University of Hawaii at Manoa, Honolulu, HI 96822, USA
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Toxins 2012, 4(11), 1082-1119; https://doi.org/10.3390/toxins4111082
Received: 14 September 2012 / Revised: 22 October 2012 / Accepted: 23 October 2012 / Published: 1 November 2012
(This article belongs to the Special Issue Novel Properties of Well-Characterized Toxins)
Scorpion toxins have been central to the investigation and understanding of the physiological role of potassium (K+) channels and their expansive function in membrane biophysics. As highly specific probes, toxins have revealed a great deal about channel structure and the correlation between mutations, altered regulation and a number of human pathologies. Radio- and fluorescently-labeled toxin isoforms have contributed to localization studies of channel subtypes in expressing cells, and have been further used in competitive displacement assays for the identification of additional novel ligands for use in research and medicine. Chimeric toxins have been designed from multiple peptide scaffolds to probe channel isoform specificity, while advanced epitope chimerization has aided in the development of novel molecular therapeutics. Peptide backbone cyclization has been utilized to enhance therapeutic efficiency by augmenting serum stability and toxin half-life in vivo as a number of K+-channel isoforms have been identified with essential roles in disease states ranging from HIV, T-cell mediated autoimmune disease and hypertension to various cardiac arrhythmias and Malaria. Bioengineered scorpion toxins have been monumental to the evolution of channel science, and are now serving as templates for the development of invaluable experimental molecular therapeutics. View Full-Text
Keywords: scorpion; peptide; toxin; potassium (K+) channel; bioengineering; probe; chimera; cyclotide; molecular therapeutic scorpion; peptide; toxin; potassium (K+) channel; bioengineering; probe; chimera; cyclotide; molecular therapeutic
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Bergeron, Z.L.; Bingham, J.-P. Scorpion Toxins Specific for Potassium (K+) Channels: A Historical Overview of Peptide Bioengineering. Toxins 2012, 4, 1082-1119.

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