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去酰基胃饥饿素:一种具有代谢活性的肽。

Des-acyl ghrelin: a metabolically active peptide.

作者信息

Delhanty Patric J, Neggers Sebastian J, van der Lely Aart J

机构信息

Department of Medicine, Erasmus University MC, Rotterdam, The Netherlands.

出版信息

Endocr Dev. 2013;25:112-21. doi: 10.1159/000346059. Epub 2013 Apr 25.

Abstract

Unacylated ghrelin (UAG), or des-acyl ghrelin, is slowly fighting its way up into the field of interest that studies preproghrelin gene-encoded peptides. Long considered to be an inert degradation product of (acylated) ghrelin (AG), UAG nowadays emerges as an important hormone, separate from the other proghrelin-derived peptides, AG and obestatin. UAG appears to have its own receptor, and it can share this receptor with AG, under experimental conditions at least. An increasing number of studies suggest that UAG can act as a potent functional inhibitor of ghrelin. It can even strongly suppress ghrelin levels in obese human diabetic subjects. Moreover, UAG can improve postprandial glycemia, especially in those subjects in whom preprandial acylated ghrelin levels are high, which makes UAG, or UAG analogs strong potential candidates for the development of drugs for the treatment of metabolic disorders or other conditions in which elevated AG/UAG ratios occur, such as diabetes, obesity and Prader-Willi syndrome.

摘要

去酰基胃饥饿素(UAG),即脱酰基胃饥饿素,正在逐步进入研究前胃饥饿素原基因编码肽的热门领域。长期以来,UAG一直被认为是(酰化)胃饥饿素(AG)的惰性降解产物,而如今它已成为一种重要的激素,与其他源自胃饥饿素原的肽(AG和肥胖抑制素)不同。UAG似乎有其自身的受体,并且至少在实验条件下,它可以与AG共享该受体。越来越多的研究表明,UAG可作为胃饥饿素的有效功能抑制剂。它甚至能强烈抑制肥胖型糖尿病患者的胃饥饿素水平。此外,UAG可改善餐后血糖,尤其是在餐前酰化胃饥饿素水平较高的患者中,这使得UAG或UAG类似物成为开发治疗代谢紊乱或其他出现AG/UAG比值升高情况(如糖尿病、肥胖症和普拉德-威利综合征)药物的有力潜在候选物。

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