Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells

Peptide-based therapy against cancer is a field of great interest for biomedical developments. Since it was shown that SK3 channels promote cancer cell migration and metastatic development, we started using these channels as targets for the development of antimetastatic drugs. Particularly, tamapin...

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Veröffentlicht in:ACS medicinal chemistry letters 2020-08, Vol.11 (8), p.1627-1633
Hauptverfasser: Mayorga-Flores, Marlen, Chantôme, Aurélie, Melchor-Meneses, Carolina Monserrath, Domingo, Isabelle, Titaux-Delgado, Gustavo Alfredo, Galindo-Murillo, Rodrigo, Vandier, Christophe, del Río-Portilla, Federico
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Sprache:eng
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Zusammenfassung:Peptide-based therapy against cancer is a field of great interest for biomedical developments. Since it was shown that SK3 channels promote cancer cell migration and metastatic development, we started using these channels as targets for the development of antimetastatic drugs. Particularly, tamapin (a peptide found in the venom of the scorpion Mesobuthus tamulus) is the most specific toxin against the SK2 channel currently known. Considering this fact, we designed diverse tamapin mutants based on three different hypotheses to discover a new potent molecule to block SK3 channels. We performed in vitro studies to evaluate this new toxin derivative inhibitor of cancer cell migration. Our results can be used to generate a new tamapin-based therapy against cancer cells that express SK3 channels.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.0c00300