Chinese scientists have analyzed the high-definition three-dimensional structure of human GLP-1R
May 31, 2017 Source: Bio Valley
Window._bd_share_config={ "common":{ "bdSnsKey":{ },"bdText":"","bdMini":"2","bdMiniList":false,"bdPic":"","bdStyle":" 0","bdSize":"16"},"share":{ }};with(document)0[(getElementsByTagName('head')[0]||body).appendChild(createElement('script')) .src='http://bdimg.share.baidu.com/static/api/js/share.js?v=89860593.js?cdnversion='+~(-new Date()/36e5)]; In a new study, researchers from the iHuman Institute of Shanghai University of Science and Technology in China and the School of Pharmacy at Fudan University analyzed glucagon-like peptide-1 receptor (GLP-1R). The molecular structure. The relevant research results were published online May 17, 2017 in the journal Nature, entitled "Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators". The author of the paper is Raymond C. Stevens, the founding director of the iHuman Institute of Shanghai University of Science and Technology, and the deputy director, Professor Zhi-Jie Liu, and the professor of the School of Pharmacy of Fudan University, Professor Ming-Wei Wang.
GLP-1R is a member of the G protein-coupled receptor (GPCR) family and is a well-known drug target for type 2 diabetes . For example, several peptide drugs targeting this target are already on the market, with annual sales of billions of dollars. Worldwide, the cost associated with treating diabetes and its complications exceeds $200 billion a year. Diabetes is increasing at an alarming rate all over the world, with the most significant recent increase occurring in China.
The structure of GLP-1R is resolved when combined with a negative allosteric modulator (NAM). NAM prevents it from being activated by insertion into the depression between the helix VI and VII of GLP-1R, while the positive allosteric modulator (PAM) mainly binds to the gap between V and VI of GLP-1R. Space to activate it. “This structure is one of the highest goals of GPCR drug development,†Stevens said.
For decades, many pharmaceutical companies have been actively looking for oral small molecule drugs to replace these peptide drugs. Associate Professor Song Gaojie from the iHuman Institute of Shanghai University of Science and Technology said, "It is particularly challenging to develop small molecule drugs for them, considering the existence of multiple junctions for GPCRs that bind peptide molecules."
Professor Wang Mingwei said, "This major task started in 2002, when we were looking for small molecule antagonists of GLP-1R. Our failure experience in developing the first oral active GLP-1R antagonist Boc5 let us Conclusion: High-resolution structural biology is the preferred solution for drug-drugability."
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