A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1916-9. doi: 10.1016/j.bmcl.2007.01.045. Epub 2007 Jan 24.

Abstract

Activation of the NPY2 receptor to reduce appetite while avoiding activation of the NPY1 and NPY5 receptors that stimulate feeding provides a pharmaceutical approach to modulate food intake. The naturally occurring peptide and development candidate PYY(3-36) is a non-selective NPY1, NPY2, and NPY5 agonist of limited in vivo duration of action. N-terminal modification with 20 kDa PEG of a selective NPY2 receptor agonist peptide results in a long-acting agent that outperforms PYY(3-36) in reducing food intake in mice. The results suggest that PEGylated, selective NPY2 peptide agonists offer a significantly improved therapeutic benefit over PYY(3-36) for obesity management.

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Dose-Response Relationship, Drug
  • Drug Design
  • Eating / drug effects*
  • Feeding Behavior / drug effects*
  • Humans
  • Kinetics
  • Mice
  • Molecular Conformation
  • Peptide Fragments
  • Peptide YY / chemical synthesis*
  • Peptide YY / pharmacology*
  • Peptides / chemistry
  • Polyethylene Glycols / chemistry*
  • Protein Binding
  • Receptors, Neuropeptide Y / chemistry*

Substances

  • Peptide Fragments
  • Peptides
  • Receptors, Neuropeptide Y
  • neuropeptide Y2 receptor
  • Peptide YY
  • peptide YY (3-36)
  • Polyethylene Glycols