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Open AccessArticle

Cell Penetration Properties of a Highly Efficient Mini Maurocalcine Peptide

by Céline Tisseyre 1,2,3,†, Eloi Bahembera 1,2,3,†, Lucie Dardevet 1,2,3, Jean-Marc Sabatier 4, Michel Ronjat 1,2,3 and Michel De Waard 1,2,4,5,*
Unité Inserm U836, Grenoble Institute of Neuroscience, Université Joseph Fourier, La Tronche, Chemin Fortuné Ferrini, Bâtiment Edmond Safra, 38042 Grenoble Cedex 09, France
Labex Ion Channel Science and Therapeutics, Nice, France
Université Joseph Fourier, Grenoble, France
Inserm U1097, Parc scientifique et technologique de Luminy, 163, avenue de Luminy, 13288 Marseille cedex 09, France
Smartox Biotechnology, Biopolis, 5 Avenue du Grand Sablon, 38700 La Tronche, France
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceuticals 2013, 6(3), 320-339;
Received: 23 February 2013 / Revised: 6 March 2013 / Accepted: 7 March 2013 / Published: 18 March 2013
(This article belongs to the Special Issue Cell-penetrating Peptides 2012)
Maurocalcine is a highly potent cell-penetrating peptide isolated from the Tunisian scorpion Maurus palmatus. Many cell-penetrating peptide analogues have been derived from the full-length maurocalcine by internal cysteine substitutions and sequence truncation. Herein we have further characterized the cell-penetrating properties of one such peptide, MCaUF1-9, whose sequence matches that of the hydrophobic face of maurocalcine. This peptide shows very favorable cell-penetration efficacy compared to Tat, penetratin or polyarginine. The peptide appears so specialized in cell penetration that it seems hard to improve by site directed mutagenesis. A comparative analysis of the efficacies of similar peptides isolated from other toxin members of the same family leads to the identification of hadrucalcin’s hydrophobic face as an even better CPP. Protonation of the histidine residue at position 6 renders the cell penetration of MCaUF1-9 pH-sensitive. Greater cell penetration at acidic pH suggests that MCaUF1-9 can be used to specifically target cancer cells in vivo where tumor masses grow in more acidic environments. View Full-Text
Keywords: maurocalcine; hadrucalcin; toxin; cell penetrating peptide; F98 cells; glioma; analogs maurocalcine; hadrucalcin; toxin; cell penetrating peptide; F98 cells; glioma; analogs
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Tisseyre, C.; Bahembera, E.; Dardevet, L.; Sabatier, J.-M.; Ronjat, M.; De Waard, M. Cell Penetration Properties of a Highly Efficient Mini Maurocalcine Peptide. Pharmaceuticals 2013, 6, 320-339.

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