The discovery of neuropeptides as signaling molecules with paracrine or hormonal regulatory functions has led to trailblazing advances in physiology and fostered the characterization of numerous neuropeptide-binding G protein-coupled receptors (GPCRs) as potential drug targets. The impact on human health has been tremendous: Approximately 30% of commercial drugs act via the GPCR pathway. However, about 25% of the GPCRs encoded by the mammalian genome still lack their pharmacological identity. Searching for the orphan GPCR endogenous ligands that are likely to be neuropeptides has proved to be a formidable task. Here we describe the mass spectrometry (MS)-based technologies and experimental strategies that have been successful in achieving high-throughput characterization of endogenous peptides in nervous and endocrine systems.

Original languageEnglish (US)
Pages (from-to)579-586
Number of pages8
JournalTrends in Pharmacological Sciences
Issue number9
StatePublished - Sep 12 2015


  • bioinformatics
  • endogenous peptides
  • mass spectrometry
  • nervous system
  • quantitation
  • sequencing

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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