A scavenger peptide prevents methylglyoxal induced pain in mice

Biochim Biophys Acta Mol Basis Dis. 2017 Mar;1863(3):654-662. doi: 10.1016/j.bbadis.2016.12.001. Epub 2016 Dec 6.

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.

Keywords: Diabetic complications; Methylglyoxal; Pain; Peptide; Scavenger.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

  • Analgesics
  • Peptides, Cyclic
  • Serum Albumin
  • Pyruvaldehyde