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据Siu FY 2013年7月15日[Nature,2013,499(7459):444-449.]报道,中美学者通过合作研究,新近在国际上首次解析了胰高血糖素受体7次跨膜区域的三维结构,为抗2型糖尿病药物的研发提供了一张“精确地图”。这是G蛋白偶联受体研究领域的一个重大突破。这项研究由中国国家新药筛选中心/中国科学院上海生命科学研究院药物研究所王明伟研究员与美国Scripps研究所雷蒙德·史蒂文斯教授合作领衔。胰高血糖素与胰岛素的作用相反,是一种促进分解代谢的激素,具有很强的促进糖原分解和糖异生作用,可使血糖明显升高。胰高血糖素通过与肝肾等靶细胞表面的B型G蛋白偶联受体进行特异性结合,激活下游信号转导通路,发挥
According to a report by Siu FY on July 15, 2013 [Nature, 2013, 499 (7459): 444-449], Chinese and American scholars recently conducted a joint international study of the first seven trans-membrane glucagon receptors The three-dimensional structure of the area provides an “accurate map” for the development of anti-type 2 diabetes drugs. This is a major breakthrough in the field of G protein-coupled receptors. The study was led by Wang Mingwei, a researcher at the National New Drug Screening Center / Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, in collaboration with Professor Raymond Stevens at the Scripps Research Institute in the United States. Glucagon and insulin on the contrary, is a hormone to promote catabolism, has a strong promotion of glycogenolysis and gluconeogenesis, can significantly increase blood glucose. Glucagon specifically binds to a B-type G protein-coupled receptor on the surface of target cells such as liver and kidney to activate the downstream signal transduction pathway