Cell penetration properties of a highly efficient mini maurocalcine peptide
| Autor: | Lucie Dardevet, Eloi Bahembera, Céline Tisseyre, Michel De Waard, Jean-Marc Sabatier, Michel Ronjat |
|---|---|
| Přispěvatelé: | INSERM U836, équipe 3, Canaux calciques, fonctions et pathologies, Grenoble Institut des Neurosciences (GIN), Université Joseph Fourier - Grenoble 1 (UJF)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Joseph Fourier - Grenoble 1 (UJF)-Institut National de la Santé et de la Recherche Médicale (INSERM), Gènes HLA-DR, Autoanticorps et Microchimérisme dans la Polyarthrite Rhumatoïde et la Sclérodermie (HLA-DR), Centre National de la Recherche Scientifique (CNRS)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Aix Marseille Université (AMU), Université Joseph Fourier - Grenoble 1 (UJF)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Joseph Fourier - Grenoble 1 (UJF)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Smartox Biotechnology, Université Joseph Fourier - Grenoble 1 (UJF), Inserm, Grenoble Hospital, Région Rhône-Alpes, Aix Marseille Université (AMU)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Canepari, Marco |
| Jazyk: | angličtina |
| Rok vydání: | 2013 |
| Předmět: |
lcsh:Medicine
lcsh:RS1-441 Pharmaceutical Science Peptide F98 cells Biology Article lcsh:Pharmacy and materia medica 03 medical and health sciences maurocalcine hadrucalcin toxin cell penetrating peptide glioma analogs In vivo Drug Discovery [SDV.BBM] Life Sciences [q-bio]/Biochemistry Molecular Biology [SDV.BBM]Life Sciences [q-bio]/Biochemistry Molecular Biology [SDV.NEU] Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC] Site-directed mutagenesis 030304 developmental biology chemistry.chemical_classification 0303 health sciences lcsh:R 030302 biochemistry & molecular biology Penetration (firestop) chemistry Biochemistry Cancer cell Cell-penetrating peptide Molecular Medicine Maurocalcine [SDV.NEU]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC] Cysteine |
| Zdroj: | Pharmaceuticals Policy and Law Pharmaceuticals Policy and Law, IOS Press, 2013, 6, pp.320-339. ⟨10.3390/ph6030320⟩ Pharmaceuticals Policy and Law, 2013, 6, pp.320-339. ⟨10.3390/ph6030320⟩ Pharmaceuticals; Volume 6; Issue 3; Pages: 320-339 Pharmaceuticals, Vol 6, Iss 3, Pp 320-339 (2013) Pharmaceuticals |
| ISSN: | 1389-2827 |
| Popis: | International audience; 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 bydirected 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. |
| Databáze: | OpenAIRE |
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