Conotoxin engineering: dual pharmacophoric noradrenaline transport inhibitor/integrin binding peptide with improved stability |
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| Authors: | Dekan Zoltan Wang Ching-I Anderson Andrews Robert K Lewis Richard J Alewood Paul F |
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| Institution: | Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Queensland, Australia. |
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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. |
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