生长素
生长激素促分泌素受体
食欲
内分泌学
能量稳态
内科学
激素
受体
信号转导
生物
医学
细胞生物学
作者
Kayleigh R. McGovern,Joseph E. Darling,James L. Hougland
出处
期刊:Mini-reviews in Medicinal Chemistry
[Bentham Science]
日期:2016-02-29
卷期号:16 (6): 465-480
被引量:10
标识
DOI:10.2174/1389557515666150722101329
摘要
Ghrelin is a circulating peptide hormone involved in regulation of a wide array of physiological processes. As an endogenous ligand for growth hormone secretagogue receptor (GHSR1a), ghrelin is responsible for signaling involved in energy homeostasis, including appetite stimulation, glucose metabolism, insulin signaling, and adiposity. Ghrelin has also been implicated in modulation of several neurological processes. Dysregulation of ghrelin signaling is implicated in diseases related to these pathways, including obesity, type II diabetes, and regulation of appetite and body weight in patients with Prader-Willi syndrome. Multiple steps in the ghrelin signaling pathway are available for targeting in the development of therapeutics for these diseases. Agonists and antagonists of GHS-R1a have been widely studied and have shown varying levels of effectiveness within ghrelin-related physiological pathways. Agents targeting ghrelin directly, either through depletion of ghrelin levels in circulation or inhibitors of ghrelin O-acyltransferase whose action is required for ghrelin to become biologically active, are receiving increasing attention as potential therapeutic options. We discuss the approaches utilized to target ghrelin signaling and highlight the current challenges toward developing small-molecule agents as potential therapeutics for ghrelin-related diseases. Keywords: Diabetes, ghrelin, ghrelin O-acyltransferase, GHS-R1a receptor, membrane-bound O-acyltransferase, obesity, Prader-Willi syndrome, spiegelmer.
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