Structural basis for motilin and erythromycin recognition by motilin receptor
文献类型：期刊论文
| 作者 | You, Chongzhao6,7; Zhang, Yumu5; Xu, Youwei7; Xu, Peiyu2,7; Li, Zhen4; Li, Huadong5; Huang, Sijie1,7; Chen, Zecai6,7; Li, Jingru4; Xu, Eric3,4,5,6,7 |
| 刊名 | SCIENCE ADVANCES
 |
| 出版日期 | 2023-03-17 |
| 卷号 | 9期号:11页码:eade9020 |
| DOI | 10.1126/sciadv.ade9020 |
| 文献子类 | Article |
| 英文摘要 | Motilin is an endogenous peptide hormone almost exclusively expressed in the human gastrointestinal (GI) tract. It activates the motilin receptor (MTLR), a class A G protein-coupled receptor (GPCR), and stimulates GI motility. To our knowledge, MTLR is the first GPCR reported to be activated by macrolide antibiotics, such as erythromycin. It has attracted extensive attention as a potential drug target for GI disorders. We report two structures of Gq-coupled human MTLR bound to motilin and erythromycin. Our structures reveal the recognition mechanism of both ligands and explain the specificity of motilin and ghrelin, a related gut peptide hormone, for their respective receptors. These structures also provide the basis for understanding the different recognition modes of erythromycin by MTLR and ribosome. These findings provide a framework for understanding the phys-iological regulation of MTLR and guiding drug design targeting MTLR for the treatment of GI motility disorders. |
| WOS关键词 | GROWTH-HORMONE SECRETAGOGUE ; MOLECULAR-BASIS ; AGONIST ; BINDING ; DESENSITIZATION ; FACILITATION ; ANTIBIOTICS ; DERIVATIVES ; MECHANISM ; GENES |
| WOS研究方向 | Science & Technology - Other Topics |
| 语种 | 英语 |
| WOS记录号 | WOS:000968083500004 |
| 出版者 | AMER ASSOC ADVANCEMENT SCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309667]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Xu, Eric; Jiang, Yi |
| 作者单位 | 1.Univ Calif San Francisco, Dept Pharmaceut Chem, San Francisco, CA USA 2.MIT, McGovern Inst Brain Res, Cambridge, MA USA; 3.Lingang Lab, Shanghai 200031, Peoples R China; 4.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing, Peoples R China; 5.ShanghaiTech Univ, Sch Life Sci & Technol ogy, Shanghai 201210, Peoples R China; 6.Univ Chinese Acad Sci, Beijing 100049, Peoples R China; 7.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | You, Chongzhao,Zhang, Yumu,Xu, Youwei,et al. Structural basis for motilin and erythromycin recognition by motilin receptor[J]. SCIENCE ADVANCES,2023,9(11):eade9020. |
| APA | You, Chongzhao.,Zhang, Yumu.,Xu, Youwei.,Xu, Peiyu.,Li, Zhen.,...&Jiang, Yi.(2023).Structural basis for motilin and erythromycin recognition by motilin receptor.SCIENCE ADVANCES,9(11),eade9020. |
| MLA | You, Chongzhao,et al."Structural basis for motilin and erythromycin recognition by motilin receptor".SCIENCE ADVANCES 9.11(2023):eade9020. |
入库方式： OAI收割
来源：上海药物研究所
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