A scavenger peptide prevents methylglyoxal induced pain in mice.

Abstract

The reactive metabolite methylglyoxal (MG) has been identified as mediator of pain. Scavenging of free MG and the prevention of MG-derived post-translational modifications may provide a useful therapeutic treatment. An arginine-rich, fatty acid coupled, cyclic peptide (CycK(Myr)R4E) with high proteolytic stability and prolonged circulation was developed for the scavenging of MG. It was shown to reduce the formation of albumin-MG adducts in vitro and prevented MG-induced pain by reducing plasma MG levels through the formation of peptide-MG adducts in vivo. CycK(Myr)R4E therefore presents a promising option for the treatment of pain and other diabetic complications associated with high MG levels.

• Authors: Sebastian Brings, Thomas Fleming, Svenja De Buhr, Barbro Beijer, Thomas Lindner, Artjom Wischnjow, Zoltan Kender, Verena Peters, Stefan Kopf, Uwe Haberkorn, Walter Mier, Peter P Nawroth
• Journal: Biochimica et biophysica acta. Molecular basis of disease (Biochim Biophys Acta Mol Basis Dis) Vol. 1863 Issue 3 Pg. 654-662 (03 2017) ISSN: 0925-4439 [Print] Netherlands
• PMID: 27932057 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2016 The Authors. Published by Elsevier B.V. All rights reserved.

Chemical References

• Analgesics
• Peptides, Cyclic
• Serum Albumin
• Pyruvaldehyde

Topics

• Amino Acid Sequence
• Analgesics (blood, chemistry, pharmacokinetics, therapeutic use)
• Animals
• Mice
• Mice, Inbred C57BL
• Pain (blood, metabolism, prevention & control)
• Peptides, Cyclic (blood, chemistry, pharmacokinetics, therapeutic use)
• Pyruvaldehyde (blood, metabolism)
• Serum Albumin (metabolism)