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Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Queensland, Australia
; Tel: +3346 2982
Australian Centre for Blood Diseases, Monash University, Alfred Medical Research & Education Precinct (AMREP), Melbourne 3004, Australia
; Fax: +03-99030228
; Tel: +03-99030136
Org. Biomol. Chem., 2012,10, 5791-5794
18 Jan 2012,
26 Apr 2012
First published online
26 Apr 2012
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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Organic & Biomolecular Chemistry
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