Recent developments in ghrelin receptor ligands

Aline Moulin, Joanne Ryan, Jean Martinez, Jean Alain Fehrentz

Research output: Contribution to journalReview ArticleResearchpeer-review

54 Citations (Scopus)

Abstract

The 28-amino acid peptide ghrelin is a neuroendocrine hormone synthesized primarily in the stomach. It stimulates growth hormone secretion and appetite, thus promoting food intake and body-weight gain. The pharmacological properties of this peptide are mediated by the growth hormone secretagogue receptor type 1a (GHS-R1a). Given its wide spectrum of biological activities, it is evident that the discovery of ghrelin and its receptor has opened up many perspectives in the fields of neuroendocrine and metabolic research and has had an influence on such fields of internal medicine as gastroenterology, oncology, and cardiology. It is therefore increasingly likely that synthetic, peptidyl, and nonpeptidyl GHS-R1a ligands, acting as agonists, partial agonists, antagonists, or inverse agonists, could have both clinical and therapeutic potential. This review summarizes the various types of GHS-R1a ligands that have been described in the literature and discusses the recent progress made in this research area.

Original languageEnglish
Pages (from-to)1242-1259
Number of pages18
JournalChemMedChem
Volume2
Issue number9
DOIs
Publication statusPublished - 10 Sep 2007
Externally publishedYes

Keywords

  • Drug design
  • Ghrelin
  • GHS-R1a ligands
  • Growth hormone secretagogues
  • Peptidomimetics

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