Issue 30, 2012

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

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

Supplementary files

Article information

Article type
Communication
Submitted
18 1 2012
Accepted
26 4 2012
First published
26 4 2012

Org. Biomol. Chem., 2012,10, 5791-5794

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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