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2013年07月23日
Anti diabetes drugs had accurate maps
July 18, 2013
Evening news
The reporter yu tao ran
"This work, as is made a map of glucagon receptor precision. In the past, people only know the existence of the receptor, now we use 'positioning' clear on its atomic structure. As a result, scientists all over the world want to design and development for the target of anti diabetes drugs, becomes accurate and efficient."
Authority evening news, Beijing time today in the morning, the international academic journals published online in nature, of the Scripps research institute and national center for drug screening/unit such as Chinese academy of sciences, Shanghai institute of medicine, scientific research personnel of a cooperation results - they parse the glucagon receptor seven transmembrane region of 3 d structure, provides resistance to drug research and development of type 2 diabetes with a precise "map". It is also the first time international parsing of type B structure of G protein coupled receptors. Nature of news review, points out that the G protein coupled receptor is a major breakthrough in the field of study.
G protein coupled receptor is a large family of membrane protein receptors in the human body known collectively, is associated with many diseases, about 40% of modern drugs to these receptors as targets. In 2012, two American scientists due to their pioneering research of G protein coupled receptor was awarded the Nobel Prize in chemistry. These receptors can be divided into A, B, C, D, E, F six types, previously, the three-dimensional structure is parsed receptors are type A, type B receptor molecules form has not been solved.
According to the national center for drug screening, Chinese academy of sciences, director of the Shanghai drug researcher Wang Mingwei introduction, in 2011, he led the team with the United States of the Scripps research institute professor Raymond Stevens, and scientific research personnel, with the purpose of Denmark, the Netherlands in the "major drug discovery" national science and technology major projects and funding support, such as the United States national institutes of health began to delve into the B type of G protein coupled receptor family members - structure of glucagon receptor.
Glucagon is a hormone secreted by the islets alpha cells, fall blood sugar and insulin action, on the other hand, it can make blood sugar rise obviously. Reduce blood sugar, pancreatic secretion of glucagon increase; When blood sugar rises, glucagon secretion is reduced. Glucagon receptor is recognized, therefore, the resistance to type 2 diabetes drug targets. The glucagon receptor is not clear, however, the structure, the world is not a role in the treatment of glucagon receptor diabetes drugs.
In countries such as China and the United States joint efforts of scientific research personnel, now the glucagon receptor has finally unveiled its mysterious veil. Wang Mingwei said they choose to small molecule ligands to stable receptor structure, promote the crystal growth. With each partner research expertise and technical advantages, won a resolution of 3.4 for the first time Mr (1 = 10 to the minus 10 meters) of glucagon receptor protein crystals of seven transmembrane region and based on the crystal structure and 128 mutations receptor affinity analysis, build the receptor and the structure model of glucagon in molecular recognition. "This work, as is made a map of glucagon receptor precision. In the past, people only know the existence of the receptor, now we use 'positioning' clear on its atomic structure. As a result, scientists all over the world want to design and development for the target of anti diabetes drugs, becomes accurate and efficient." Wang Mingwei said.
Be worth what carry is, at the same time nature also published British scientists resolved another type B G protein coupled receptor - corticotrophin releasing factor receptor 1 molecular structures. The top academic journals published news commentary pointed out that the two receptors of seven transmembrane region structure parsing, marks a breakthrough in the field of G protein coupled receptor research. In the near future, a batch of on the basis of the development of new drugs is expected to come out, for the benefit of human health.
(the original title: anti diabetes drugs have a precise map)
The original link: http://news.sina.com.cn/o/2013-07-18/131927704468.shtml
(this site editor Wang Zhong one)