Moulin Aline, Ryan Joanne, Martinez Jean, Fehrentz Jean-Alain
Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, BP 1441, 34093 Montpellier Cedex, France.
ChemMedChem. 2007 Sep;2(9):1242-59. doi: 10.1002/cmdc.200700015.
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.
由28个氨基酸组成的肽类激素胃饥饿素主要在胃中合成。它刺激生长激素分泌和食欲，从而促进食物摄入和体重增加。这种肽的药理特性由1a型生长激素促分泌素受体（GHS-R1a）介导。鉴于其广泛的生物学活性，胃饥饿素及其受体的发现显然为神经内分泌和代谢研究领域开辟了许多新视角，并对胃肠病学、肿瘤学和心脏病学等内科领域产生了影响。因此，作为激动剂、部分激动剂、拮抗剂或反向激动剂的合成肽基和非肽基GHS-R1a配体越来越有可能具有临床和治疗潜力。这篇综述总结了文献中描述的各种类型的GHS-R1a配体，并讨论了该研究领域的最新进展。
