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Issue 30, 2012
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Conotoxin engineering: dual pharmacophoric noradrenaline transport inhibitor/integrin binding peptide with improved stability

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Abstract

A dual-pharmacophoric peptide was engineered by grafting the integrin binding RGD motif between the C- and N-termini of a disulfide-rich noradrenaline transporter inhibiting χ-conotoxin resulting in a stable backbone cyclized peptide. The construct maintained two independent biological activities and showed increased plasma stability with no adverse effects observed following administration to rats, highlighting the potential value of pharmacophore grafting into constrained peptide scaffolds.

Graphical abstract: Conotoxin engineering: dual pharmacophoric noradrenaline transport inhibitor/integrin binding peptide with improved stability

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Publication details

The article was received on 18 Jan 2012, accepted on 26 Apr 2012 and first published on 26 Apr 2012


Article type: Communication
DOI: 10.1039/C2OB25133G
Citation: Org. Biomol. Chem., 2012,10, 5791-5794
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    Conotoxin engineering: dual pharmacophoric noradrenaline transport inhibitor/integrin binding peptide with improved stability

    Z. Dekan, C. A. Wang, R. K. Andrews, R. J. Lewis and P. F. Alewood, Org. Biomol. Chem., 2012, 10, 5791
    DOI: 10.1039/C2OB25133G

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