Recent developments in ghrelin receptor ligands |
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Authors: | Moulin Aline Ryan Joanne Martinez Jean Fehrentz Jean-Alain |
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Affiliation: | Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, BP 1441, 34093 Montpellier Cedex, France. |
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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. |
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Keywords: | drug design ghrelin GHS‐R1a ligands growth hormone secretagogues peptidomimetics |
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