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Traditionally viewed as a source of toxic compounds, animal venoms are in fact a large reservoir of biologically active peptides that can be used for therapeutic applications. This chapter deals with the frontrunners in the search for therapeutic applications amongst scorpion-venom-derived peptides. Areas covered include: 1) the potential use of antimicrobial and potassium channel blocking peptides as drug leads; 2) the utility of small disulfide-rich proteins as pharmaceutical tools for tumor labeling and as drug carriers; and 3) the use of toxin scaffolds to engineer pharmaceutically tractable and stable mimetics of larger proteins. These frontrunners belong to the three best known structural classes of scorpion-venom-derived peptides. Here it is argued that the vast number of non-canonical scorpion-venom components revealed by high-throughput bioprospecting promise to greatly expand the number of potential drug leads from scorpion venoms.

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