氧辛托莫杜林 - - 过去,现在和未来
Jens Juul Holst1, Mette M Rosenkilde2
1The NovoNordisk Foundation Center for Basic Metabolic Research, Denmark; Department of Biomedical Sciences, the Panum institute, University of Copenhagen, Denmark.
Peptides
|April 5, 2025
概括
一种肠道的oxyntomodulin显示出治疗代谢功能障碍相关的脂肪性肝病 (MASLD) 的前景. 它的双重作用激发了新的葡萄糖-GLP-1共激素剂,用于减肥和减少肝脏脂肪.
科学领域:
- 内分泌学 在内分泌学.
- 胃肠病学 胃肠病学
- 代谢疾病 代谢疾病
背景情况:
- 葡萄糖的胃肠道起源是由含有类似葡萄糖的免疫活性的L细胞暗示的.
- 在L细胞中存在glicentin和oxyntomodulin,两者都含有完整的葡萄糖序列.
- 氧辛托莫杜林 (oxyntomodulin) 是一种glicentin片段,它与葡萄糖和GLP-1受体相互作用,影响食欲和食物摄入.
研究的目的:
- 探索oxyntomodulin及其衍生物的治疗潜力.
- 为了研究葡萄糖-GLP-1共激剂在治疗代谢障碍中的疗效.
- 评估这些协同激动剂对减肥和肝硬化症的影响.
主要方法:
- 对与葡萄糖和GLP-1受体的相互作用的分析.
- 人类研究对oxyntomodulin对食欲和食物摄入的影响.
- 长期作用的葡萄糖-GLP-1共激素的临床开发.
主要成果:
- 牛津托莫杜林在人类中显示出食欲和食物摄入的抑制.
- 葡萄糖-GLP-1共激素剂可以实现增量减肥.
- 协同激素刺激肝脂代谢,在肝硬化症中显示出有效性.
结论:
- 氧辛托莫杜林的特性激发了有前途的葡萄糖-GLP-1协同激动剂的开发.
- 这些协同激动剂为体重管理和代谢健康提供了双重治疗方法.
- 有可能有效治疗与代谢功能障碍相关的脂肪性肝病 (MASLD).
相关概念视频
01:24Glucagon-like Receptor Agonists
272
Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
272
01:40Hormonal Regulation
43.0K
Hormones regulate a significant portion of digestion through activation of the neuroendocrine system. The neuroendocrine system of digestion contains many different hormones all with multiple functions that are both, directly and indirectly, involved in digestion.
43.0K
01:27Glucose Transporters
22.2K
Glucose transporters facilitate the transport of glucose across the cell membrane. In addition to glucose, some glucose transporters can also aid the movement of other hexoses such as fructose, mannose, and galactose.
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
22.2K
01:27Transducer Mechanism: Enzyme-Linked Receptors
2.3K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.3K
01:30Regulation of Food Intake
155
Short-term regulation of food intake primarily involves neural signals from the gastrointestinal (GI) tract, blood nutrient levels, and GI tract hormones. Communication between the gut and brain via vagal nerve fibers plays a significant role in evaluating the contents of the gut. Clinical studies have shown that protein ingestion produces a more prolonged response in these nerve fibers compared to an equivalent amount of glucose. Additionally, the activation of stretch receptors caused by GI...
155
01:23Transcellular Transport of Solutes
3.3K
Transcellular transport of solutes is the movement of substances like monosaccharides and amino acids through polarized cells. This transport mechanism is primarily seen in epithelial and endothelial cells aided by membrane transport proteins such as channels and transporters. The tight junctions between these cells confine the membrane proteins to the two sides of the cell. The epithelial cells have distinct apical and basolateral domains. In contrast, the endothelial cells show the luminal...
3.3K