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D-Maurocalcine, a pharmacologically inert efficient cell-penetrating peptide analogue.: Cell Penetrating D-Maurocalcine Peptide

Abstract : Maurocalcine has been the first demonstrated animal toxin acting as a cell-penetrating peptide. Although it possesses competitive advantages, its use as a cell-penetrating peptide (CPP) requires that analogues be developed that lack its characteristic pharmacological activity on ryanodine-sensitive calcium channels without affecting its cell-penetrating and vector efficiencies. Here, we present the synthesis, three-dimensional (1)H NMR structure, and activity of D-maurocalcine. We demonstrate that it possesses all of the desired features for an excellent CPP: preserved structure, lack of pharmacological action, conserved vector properties, and absence of cell toxicity. This is the first report of a folded/oxidized animal toxin in its D-diastereomer conformation for use as a CPP. The protease resistance of this new peptide analogue, combined with its efficient cell penetration at concentrations devoid of cell toxicity, suggests that D-maurocalcine should be an excellent vector for in vivo applications.
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Submitted on : Thursday, July 7, 2011 - 3:39:09 PM
Last modification on : Sunday, May 31, 2020 - 10:51:09 AM
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Cathy Poillot, Kaouthar Dridi, Hicham Bichraoui, Julien Pêcher, Sébastien Alphonse, et al.. D-Maurocalcine, a pharmacologically inert efficient cell-penetrating peptide analogue.: Cell Penetrating D-Maurocalcine Peptide. Journal of Biological Chemistry, American Society for Biochemistry and Molecular Biology, 2010, 285 (44), pp.34168-80. ⟨10.1074/jbc.M110.104919⟩. ⟨inserm-00587800⟩

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