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CPP-Ts: a new intracellular calcium channel modulator and a promising tool for drug delivery in cancer cells.

Bárbara Bruna Ribeiro de Oliveira-MendesCarolina Campolina Rebello HortaAnderson Oliveira do CarmoGabriela Lago BiscotoDouglas Ferreira Sales-MedinaHortênsia Gomes LealPedro Ferreira Pinto Brandão-DiasSued Eustáquio Mendes MirandaCarla Jeane AguiarValbert Nascimento CardosoAndré Luís Branco de BarrosCarlos Chávez-OlortéguiM Fátima LeiteEvanguedes Kalapothakis
Published in: Scientific reports (2018)
Scorpion sting envenoming impacts millions of people worldwide, with cardiac effects being one of the main causes of death on victims. Here we describe the first Ca2+ channel toxin present in Tityus serrulatus (Ts) venom, a cell penetrating peptide (CPP) named CPP-Ts. We show that CPP-Ts increases intracellular Ca2+ release through the activation of nuclear InsP3R of cardiomyocytes, thereby causing an increase in the contraction frequency of these cells. Besides proposing a novel subfamily of Ca2+ active toxins, we investigated its potential use as a drug delivery system targeting cancer cell nucleus using CPP-Ts's nuclear-targeting property. To this end, we prepared a synthetic CPP-Ts sub peptide14-39 lacking pharmacological activity which was directed to the nucleus of specific cancer cell lines. This research identifies a novel subfamily of Ca2+ active toxins and provides new insights into biotechnological applications of animal venoms.
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