升糖素及ＧＬＰ－１受體之共促效劑农业专利-农业学术服务平台

发明人:: CARRINGTON, PAUL E.,凯林顿　保罗Ｅ,凱林頓　保羅Ｅ,DENG, QIAOLIN,邓　巧临,鄧　巧臨,NARGUND, RAVI,纳格恩　瑞维,納格恩　瑞維,PALANI, ANANDAN,帕拉尼　安纳丹,帕拉尼　安納丹,TUCKER, THOMAS JOSEPH,图克　汤马士　乔瑟夫,圖克　湯馬士　喬瑟夫,WU, CHENGWEI,吴　成威,吳　成威,BIANCHI, ELIS,凯林顿保罗E,凱林頓保羅E,邓巧临,鄧巧臨,纳格恩瑞维,納格恩瑞維,帕拉尼安纳丹,帕拉尼安納丹,图克汤马士乔瑟夫,圖克湯馬士喬瑟夫,吴成威,吳成威

摘要：: Described are peptide analogs of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have relatively balanced agonist activity at the glucagon-like peptide 1 (GLP-1) receptor and the glucagon (GCG) receptor, and the use of such GLP-1 receptor/GCG receptor co-agonists for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.本發明描述升糖素之胜肽類似物，其業經修飾以抵抗藉由二肽基肽酶IV(dipeptidyl peptidase IV；DPP-IV)之裂解及失活作用，並可增加該胜肽類似物之活體內半衰期，同時使胜肽類似物在升糖素樣肽1(GLP-1)受體及升糖素(GCG)受體處具有相對平衡之促效劑活性，及一種此等GLP-1受體/GCG受體共促效劑於治療代謝疾病(諸如糖尿病、非酒精性脂肪肝病(non-alcoholic fatty liver disease；NAFLD)、非酒精性脂肪肝炎(non-alcoholic steatohepatitis；NASH)及肥胖)之用途。