| 取代环丁烷结构的非肽类胰高血糖素样肽-1受体激动剂 |
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| 引用本文： | 刘青,何敏,周彩红,王明伟.取代环丁烷结构的非肽类胰高血糖素样肽-1受体激动剂[J].生命科学,2012(7):626-633. |
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| 作者姓名： | 刘青 何敏 周彩红 王明伟 |
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| 作者单位： | 中国科学院上海药物研究所／国家新药筛选中心,上海201203 |
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| 基金项目： | 国家重大科技专项“十一五”和“十二五”计划（2009-ZX09302-001,2012ZX09304-011）; 中国科学院重大项目（KSCX1-YW-02-2）和方向性项目（KSCX2-YW-R-17）; 上海市科委项目（11DZ2292200）; 诺和诺德-中国科学院研究基金 |
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| 摘 要： | 应用胰高血糖素样肽-1（glucagon-like peptide-1,GLP-1）及其类似物治疗2型糖尿病是代谢性疾病研究领域近年来的热点,尤其是胰高血糖素样肽-1独特的作用机制倍受业界的关注。它能同时作用于2型糖尿病的多个发病环节,在有效降低血糖的同时,避免低血糖的发生并能减轻体重。但这类药物因其多肽性质而存在诸多的使用限制（如需反复注射）。简要介绍一类取代环丁烷结构的新型非肽类胰高血糖素样肽-1受体小分子激动剂的发现过程、基本药理学特征和体内抗糖尿病和抗肥胖症效应。
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| 关 键 词： | 胰高血糖素样肽-1 环丁烷结构 糖尿病 |
Substituted cyclobutane derivatives as non-peptidic GLP-1 receptor agonists |
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| LIU Qing,HE Min,ZHOU Cai-Hong,WANG Ming-Wei.Substituted cyclobutane derivatives as non-peptidic GLP-1 receptor agonists[J].Chinese Bulletin of Life Sciences,2012(7):626-633. |
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| Authors: | LIU Qing HE Min ZHOU Cai-Hong WANG Ming-Wei |
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| Institution: | (The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China) |
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| Abstract: | Application of glucagon-like peptide-1 （GLP-1） to treat type 2 diabetes has become a focal point in the study of metabolic diseases in recent years. Of particular interest is the unique mechanisms of action relative to GLP-1. It exerts multiple effects on the pathogenesis of type 2 diabetes. While effectively lowering blood glucose levels, it does not cause hypoglycemia but reduces body weight. However, GLP-1 and its peptidic mimetics require frequent injections that limits their wide use. This paper briefly reviews the discovery and pharmacological characterization of a class of novel cyclobutane derivatives as non-peptidic GLP-1 receptor agonists including in vivo efficacies on diabetes and obesity. |
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| Keywords: | glucagon-like peptide-1 （GLP-1） cyclobutane derivatives diabetes |
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