Delhanty Patric J D, Neggers Sebastian J, van der Lely Aart J
Department of Internal Medicine, Erasmus MC, Rotterdam, The Netherlands.
Front Horm Res. 2014;42:163-74. doi: 10.1159/000358345. Epub 2014 Apr 7.
The peptides ghrelin (or acyl ghrelin; AG), des-acyl ghrelin (DAG) and obestatin are all encoded by the prepro-ghrelin gene that is expressed predominantly in the stomach. Compared with ghrelin and obestatin, DAG has not received a great amount of attention. DAG has long been considered an inert degradation product of AG. Recent evidence, however, indicates that DAG behaves like a separate hormone. Therefore, it is believed that DAG must activate its own receptor, and that it may also interact with AG at this receptor. DAG can act together with AG, can antagonize AG and seems to have AG-independent effects. Of potential clinical importance is that an increasing number of studies suggest that DAG is a functional inhibitor of AG. Therefore, DAG or DAG analogs are being trialed in early clinical studies for treatment of metabolic disorders such as diabetes, obesity and Prader-Willi syndrome.
肽类物质胃饥饿素(或酰基化胃饥饿素;AG)、去酰基胃饥饿素(DAG)和肥胖抑制素均由主要在胃中表达的前胃饥饿素基因编码。与胃饥饿素和肥胖抑制素相比,DAG尚未受到大量关注。长期以来,DAG一直被认为是AG的惰性降解产物。然而,最近的证据表明,DAG的行为类似于一种独立的激素。因此,人们认为DAG必须激活其自身的受体,并且它也可能在该受体处与AG相互作用。DAG可以与AG共同发挥作用,可以拮抗AG,并且似乎具有不依赖于AG的作用。具有潜在临床重要性的是,越来越多的研究表明DAG是AG的功能性抑制剂。因此,DAG或DAG类似物正在早期临床研究中进行试验,用于治疗代谢紊乱,如糖尿病、肥胖症和普拉德-威利综合征。