The use of tripeptides for lead discovery of 5-HT4 receptor ligands

Protein Pept Lett. 2009;16(7):805-9. doi: 10.2174/092986609788681805.

Abstract

A series of 30 tripeptides were synthesized and tested as novel 5-HT4 receptor ligands. Receptor binding assays showed that a subset of compounds had reasonable potency relative to the agonists serotonin and 5-methoxytryptamine. Structure-activity analyses and molecular docking have highlighted avenues for further synthetic work.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Biogenic Amines / metabolism
  • Drug Discovery*
  • Humans
  • Ligands
  • Models, Molecular
  • Oligopeptides / chemistry*
  • Oligopeptides / metabolism*
  • Receptors, Serotonin, 5-HT4 / chemistry
  • Receptors, Serotonin, 5-HT4 / metabolism*

Substances

  • Biogenic Amines
  • Ligands
  • Oligopeptides
  • Receptors, Serotonin, 5-HT4