Neuropeptide Y receptors: ligand binding and trafficking suggest novel approaches in drug development

J Pept Sci. 2011 Apr;17(4):233-46. doi: 10.1002/psc.1357. Epub 2011 Feb 24.


NPY, PYY and PP constitute the so-called NPY hormone family, which exert its biological functions in humans through YRs (Y₁, Y₂, Y₄ and Y₅). Systematic modulation of YR function became important as this multireceptor/multiligand system is known to mediate various essential physiological key functions and is involved in a variety of major human diseases such as epilepsy, obesity and cancer. As several YRs have been found to be overexpressed on different types of malignant tumors they emerge as promising target in modern drug development. Here, we summarize the current understanding of YRs function and the molecular mechanisms of ligand binding and trafficking. We further address recent advances in YR-based drug design, the development of promising future drug candidates and novel approaches in YR-targeted tumor diagnostics and therapy opportunities.

Publication types

  • Review

MeSH terms

  • Drug Design*
  • Humans
  • Ligands*
  • Molecular Structure
  • Neoplasms / drug therapy
  • Neuropeptide Y / genetics
  • Neuropeptide Y / metabolism
  • Obesity / drug therapy
  • Pancreatic Polypeptide / genetics
  • Pancreatic Polypeptide / metabolism
  • Peptide YY / genetics
  • Peptide YY / metabolism
  • Protein Isoforms / genetics
  • Protein Isoforms / metabolism
  • Receptors, Neuropeptide Y / genetics
  • Receptors, Neuropeptide Y / metabolism*


  • Ligands
  • Neuropeptide Y
  • Protein Isoforms
  • Receptors, Neuropeptide Y
  • Peptide YY
  • Pancreatic Polypeptide