Conotoxin engineering: Dual pharmacophoric noradrenaline transport inhibitor/integrin binding peptide with improved stability

Zoltan Dekan, Ching I Anderson Wang, Robert K. Andrews, Richard J Lewis, Paul F Alewood

Research output: Contribution to journalArticleOtherpeer-review

10 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)5791-5794
Number of pages4
JournalOrganic and Biomolecular Chemistry
Volume10
Issue number30
DOIs
Publication statusPublished - 14 Aug 2012

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