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Peptides and Peptidomimetics as Potential Antiobesity Agents: Overview of Current Status

机译:肽和拟肽作为潜在的减肥药:现状概述

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摘要

There is a high occurrence of obesity worldwide without many new medications being approved for its treatment. Therefore, there is an urgent need to introduce new approaches for treating obesity. Bioactive peptides have been used to treat metabolic disorders- such as type-2 diabetes and obesity; while also possessing anti-oxidant, anti-inflammatory, anti-microbial, and anti-viral properties. However, the development of these peptides has taken backstage due to their size, reduced stability, poor delivery and bioavailability, fast rate of degradation etc. But with the emergence of newer techniques for multifunctional peptides, mimetics, peptide analogs, and aptamers, there is a sudden revival in this therapeutic field. An increased attention is required for development of the natural peptides from food and marine sources which can mimic the function of mediators involved in weight management to avoid obesity. Herein, the search for the structures of anti-obesity peptides was carried out in order to establish their potential for drug development in future. An extensive search for the current status of endogenous, food and marine peptides, with reference to novel and interesting experimental approaches based on peptidomimetics for controlling obesity, was performed. Apolipoprotein A-I (apoA-I), melanocortin-4 receptor (MC4R)-specific agonist, GLP-1 dual and triple agonists, neuropeptides and prolactin-releasing peptide mimetics were specifically examined for their anti-obesity role. Novel peptides, mimetics, and synthesis interventions are transpiring and might offer safer alternatives for otherwise scarcely available safe antiobesity drug. A deeper understanding of peptides and their chemistry through the use of peptide engineering can be useful to overcome the disadvantages and select best mimetics and analogs for treatment in future.
机译:在世界范围内,肥胖症的发生率很高,而许多新药物均未获批准用于治疗肥胖症。因此,迫切需要引入治疗肥胖的新方法。生物活性肽已用于治疗代谢性疾病,例如2型糖尿病和肥胖症;同时还具有抗氧化,抗炎,抗微生物和抗病毒的特性。但是,由于这些肽的大小,稳定性降低,递送和生物利用度差,降解速度快等原因,这些肽的开发已进入后台。但是随着多功能肽,模拟物,肽类似物和适体的更新技术的出现,在这个治疗领域突然复兴。从食物和海洋来源开发天然肽需要更多的关注,这种肽可以模仿体重控制中涉及的介体的功能,以避免肥胖。在本文中,进行抗肥胖肽的结构的搜索以建立其将来在药物开发中的潜力。参考基于肽模拟物控制肥胖的新颖有趣的实验方法,对内源性,食品和海洋肽的现状进行了广泛的研究。载脂蛋白A-I(apoA-I),黑皮质素4受体(MC4R)特异性激动剂,GLP-1双和三重激动剂,神经肽和催乳素释放肽模拟物的抗肥胖作用已得到专门研究。新型肽,模拟物和合成干预措施正在普及,并可能为原本很少可获得的安全性抗肥胖药提供更安全的替代品。通过使用肽工程技术对肽及其化学方法进行更深入的了解可能有助于克服缺点,并选择最佳的模拟物和类似物进行将来的治疗。

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