Identifying Receptors for Neuropeptides and Peptide Hormones: Challenges and Recent Progress

Intercellular signaling events mediated by neuropeptides and peptide hormones represent important targets for both basic science drug discovery. For many bioactive peptides, the protein receptors that transmit information across receiving cell membrane are not known, severely limiting these pathways as potential therapeutic targets. Identifying receptor(s) a given of interest is complicated several factors. Most notably, cell–cell peptides generated through dynamic biosynthetic pathways, can act on different families receptor proteins, participate in complex ligand–receptor interactions extend beyond simple one-to-one archetype. Here, we discuss recent methodological advances to identify partners peptides. Recent efforts have centered methods candidate via transcript expression, match peptide–receptor pairs high throughput screening, capture direct using chemical probes. Future applications identification approaches discussed here, well technical advancements address their limitations, promise lead greater understanding how cells communicate deliver physiologies. Importantly, such will likely provide novel treatment human diseases within central nervous endocrine systems.