Metformin is a novel suppressor for transforming growth factor (TGF)-beta 1
文献类型：期刊论文
| 作者 | Xiao, Han1,2,3; Zhang, Jianshu1,2,3; Xu, Zhonghe4; Feng, Yenan1,2,3; Zhang, Mingliang1,2,3; Liu, Jianli5; Chen, Ruifei1,2,3; Shen, Jing1,2,3; Wu, Jimin1,2,3; Lu, Zhizhen1,2,3 |
| 刊名 | SCIENTIFIC REPORTS
 |
| 出版日期 | 2016-06-28 |
| 卷号 | 6 |
| 英文摘要 | Metformin is a widely used first-line antidiabetic drug that has been shown to protect against a variety of specific diseases in addition to diabetes, including cardiovascular disorders, polycystic ovary syndrome, and cancer. However, the precise mechanisms underlying the diverse therapeutic effects of metformin remain elusive. Here, we report that transforming growth factor-beta 1 (TGF-beta 1), which is involved in the pathogenesis of numerous diseases, is a novel target of metformin. Using a surface plasmon resonance-based assay, we identified the direct binding of metformin to TGF-beta 1 and found that metformin inhibits [I-125]-TGF-beta 1 binding to its receptor. Furthermore, based on molecular docking and molecular dynamics simulations, metformin was predicted to interact with TGF-beta 1 at its receptor-binding domain. Single-molecule force spectroscopy revealed that metformin reduces the binding probability but not the binding force of TGF-beta 1 to its type II receptor. Consequently, metformin suppresses type II TGF-beta 1 receptor dimerization upon exposure to TGF-beta 1, which is essential for downstream signal transduction. Thus, our results indicate that metformin is a novel TGF-beta suppressor with therapeutic potential for numerous diseases in which TGF-beta 1 hyperfunction is indicated. |
| 收录类别 | SCI |
| 语种 | 英语 |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/35529]  |
| 专题 | 化学研究所_分子纳米结构与纳米技术实验室 |
| 作者单位 | 1.Peking Univ, Hosp 3, Inst Vasc Med, Beijing 100191, Peoples R China 2.Peking Univ, Acad Adv Interdisciplinary Studies, Key Lab Cardiovasc Mol Biol & Regulatory Peptides, Minist Hlth,Key Lab Mol Cardiovasc Sci,Minist Edu, Beijing 100191, Peoples R China 3.Beijing Key Lab Cardiovasc Receptors Res, Beijing 100191, Peoples R China 4.Chinese Acad Sci, Inst High Energy Phys, Key Lab Biomed Effects Nanomat & Nanosafety, Beijing 100049, Peoples R China 5.Chinese Acad Sci, Key Lab Mol Nanostruct & Nanotechnol, Beijing Natl Lab Mol Sci, Inst Chem, Beijing 100190, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xiao, Han,Zhang, Jianshu,Xu, Zhonghe,et al. Metformin is a novel suppressor for transforming growth factor (TGF)-beta 1[J]. SCIENTIFIC REPORTS,2016,6. |
| APA | Xiao, Han.,Zhang, Jianshu.,Xu, Zhonghe.,Feng, Yenan.,Zhang, Mingliang.,...&Zhang, Youyi.(2016).Metformin is a novel suppressor for transforming growth factor (TGF)-beta 1.SCIENTIFIC REPORTS,6. |
| MLA | Xiao, Han,et al."Metformin is a novel suppressor for transforming growth factor (TGF)-beta 1".SCIENTIFIC REPORTS 6(2016). |
入库方式： OAI收割
来源：化学研究所
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