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Pharmaceuticals 2013, 6(3), 320-339; doi:10.3390/ph6030320
Article

Cell Penetration Properties of a Highly Efficient Mini Maurocalcine Peptide

1,2,3,†, 1,2,3,†, 1,2,3, 4, 1,2,3 and 1,2,4,5,*
Received: 23 February 2013; in revised form: 6 March 2013 / Accepted: 7 March 2013 / Published: 18 March 2013
(This article belongs to the Special Issue Cell-penetrating Peptides)
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Abstract: 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.
Keywords: maurocalcine; hadrucalcin; toxin; cell penetrating peptide; F98 cells; glioma; analogs maurocalcine; hadrucalcin; toxin; cell penetrating peptide; F98 cells; glioma; analogs
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

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(3):320-339.

Chicago/Turabian Style

Tisseyre, Céline; Bahembera, Eloi; Dardevet, Lucie; Sabatier, Jean-Marc; Ronjat, Michel; De Waard, Michel. 2013. "Cell Penetration Properties of a Highly Efficient Mini Maurocalcine Peptide." Pharmaceuticals 6, no. 3: 320-339.



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