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

Marlen Mayorga-Flores, Aurélie Chantôme, Carolina Monserrath Melchor-Meneses, Isabelle Domingo, Gustavo Alfredo Titaux-Delgado, Rodrigo Galindo-Murillo, Christophe Vandier, Federico Del Río-Portilla

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)1627-1633
Number of pages7
JournalACS Medicinal Chemistry Letters
Volume11
Issue number8
DOIs
StatePublished - Aug 13 2020
Externally publishedYes

Keywords

  • MDA-MB-435s
  • migration cells
  • scorpion toxins
  • SK2 channels
  • SK3 channels
  • tamapin

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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