中国科技核心期刊
CN:31-1600/Q
ISSN:1004-0374
“健康与疾病的免疫”国际学术研讨会通知      关于有网站冒充本刊网站的声明
《生命科学》 2012, 24(7): 626-633
取代环丁烷结构的非肽类胰高血糖素样肽-1受体激动剂
刘 青,何 敏,周彩红,王明伟*
(中国科学院上海药物研究所/国家新药筛选中心,上海 201203)
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。
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
LIU Qing, HE Min, ZHOU Cai-Hong, WANG Ming-Wei*
(The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China)
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.
Key words: glucagon-like peptide-1 (GLP-1); cyclobutane derivatives; diabetes
 
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