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Inventing Liraglutide, a Glucagon-Like Peptide-1 Analogue, for the Treatment of Diabetes and Obesity.
ACS Pharmacology & Translational Science Pub Date : 2019-08-20 , DOI: 10.1021/acsptsci.9b00048
Lotte Bjerre Knudsen 1
Affiliation  

Glucagon-like peptide-1 (GLP-1) has been in focus since the early 1980s as a long looked for incretin hormone, released from the gastrointestinal tract and with an important effect on glucose-dependent insulin secretion, providing efficient glucose lowering, with little risk for hypoglycemia. The enzyme dipeptidyl peptidase-4 (DPP-4) degrades GLP-1 very fast, and the remaining metabolite is cleared rapidly by the kidneys. Liraglutide is a fatty acid acylated analogue of GLP-1 that provides efficacy for 24 h/day. The mechanism of action for liraglutide is reviewed in detail with focus on pancreatic efficacy and safety, thyroid safety, and weight loss mechanism. Evolving science hypothesizes that GLP-1 has important effects on atherosclerosis, relevant for the cardiovascular benefit seen in the treatment of diabetes and obesity. Also, GLP-1 may be relevant in neurodegenerative diseases.

中文翻译:

发明了胰高血糖素样肽1类似物利拉鲁肽,用于治疗糖尿病和肥胖症。

自1980年代初以来,胰高血糖素样肽1(GLP-1)一直是人们关注的焦点,因为人们一直在寻找从胃肠道释放的肠降血糖素激素,它对葡萄糖依赖性胰岛素的分泌具有重要作用,可以有效降低血糖,低血糖的风险很小。二肽基肽酶-4(DPP-4)酶可以非常快速地降解GLP-1,并且肾脏可以快速清除残留的代谢产物。利拉鲁肽是GLP-1的脂肪酸酰化类似物,每天提供24小时的功效。对利拉鲁肽的作用机理进行了详细的综述,重点是胰腺功效和安全性,甲状腺安全性以及减肥机理。不断发展的科学假设认为,GLP-1对动脉粥样硬化具有重要作用,与治疗糖尿病和肥胖症所产生的心血管益处相关。还,
更新日期:2019-08-20
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