GLP-1/glucagon receptor co-agonism for treatment of obesity.
GLP-1/glucagon receptor co-agonism for treatment of obesity.
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DOI：
10.1007/s00125-017-4354-8
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发表时间：
2017-10
期刊：
影响因子：
8.2
通讯作者：
Tschöp MH
中科院分区：
文献类型：
--
作者：
Sánchez-Garrido MA;Brandt SJ;Clemmensen C;Müller TD;DiMarchi RD;Tschöp MH
在相对较短的时间内，肥胖和 2 型糖尿病已成为全球社会的巨大医疗和经济负担。肥胖患病率的普遍上升会带来代谢后果，同时其他疾病的发生率也会增加，例如糖尿病、癌症和心血管并发症。肥胖和 2 型糖尿病共同构成了更可预防的过早死亡原因之一，识别新型、安全且有效的抗肥胖药物至关重要。治疗肥胖的药理学尝试取得了有限的成功，并具有显着的副作用，使得减肥手术成为目前唯一能大幅改善体重的疗法。新型单分子多功能肽已成为增强代谢功效和恢复正常体重最有前途的药物方法之一。在这篇综述中，我们将主要关注在胰高血糖素和胰高血糖素样肽-1 受体上发挥药理学作用的双重激动剂的发现和转化相关性。此类肽已进入临床评估阶段，并激发了人们对多种相关方法的追求，以在单分子内实现多药治疗。本文的在线版本 (doi:10.1007/s00125-017-4354-8) 包含可供下载的图幻灯片，可供授权用户使用。
Over a relatively short period, obesity and type 2 diabetes have come to represent a large medical and economic burden to global societies. The epidemic rise in the prevalence of obesity has metabolic consequences and is paralleled by an increased occurrence of other diseases, such as diabetes, cancer and cardiovascular complications. Together, obesity and type 2 diabetes constitute one of the more preventable causes of premature death and the identification of novel, safe and effective anti-obesity drugs is of utmost importance. Pharmacological attempts to treat obesity have had limited success, with notable adverse effects, rendering bariatric surgery as the only current therapy for substantially improving body weight. Novel unimolecular, multifunctional peptides have emerged as one of the most promising medicinal approaches to enhance metabolic efficacy and restore normal body weight. In this review, we will mainly focus on the discovery and translational relevance of dual agonists that pharmacologically function at the receptors for glucagon and glucagon-like peptide-1. Such peptides have advanced to clinical evaluation and inspired the pursuit of multiple related approaches to achieving polypharmacy within single molecules. The online version of this article (doi:10.1007/s00125-017-4354-8) contains a slide of the figure for download, which is available to authorised users.
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影响因子：
4.8
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