Issue 30, 2012
From the journal:

Organic & Biomolecular Chemistry

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

Zoltan Dekan,a   Ching-I Anderson Wang,a   Robert K. Andrews,b   Richard J. Lewisa  and  Paul F. Alewooda  

a Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Queensland, Australia
E-mail: p.alewood@imb.uq.edu.au
Tel: +3346 2982

b Australian Centre for Blood Diseases, Monash University, Alfred Medical Research & Education Precinct (AMREP), Melbourne 3004, Victoria, Australia
E-mail: rob.andrews@monash.edu
Fax: +03-99030228
Tel: +03-99030136

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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Article information

DOI
https://doi.org/10.1039/C2OB25133G
Article type
Communication
Submitted
18 Jan 2012
Accepted
26 Apr 2012
First published
26 Apr 2012

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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