• GPCR;
  • NPY;
  • YR;
  • structure-activity relationship;
  • internalization;
  • drug development;
  • receptor trafficking


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. Copyright © 2011 European Peptide Society and John Wiley & Sons, Ltd.