RepSox, a small molecule inhibitor of the TGF beta receptor, induces brown adipogenesis and browning of white adipocytes
文献类型：期刊论文
| 作者 | Tu, Wan-zhi2,3,4; Fu, Yan-bin1,2; Xie, Xin1,2,3,4
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2019-12-01 |
| 卷号 | 40期号:12页码:1523-1531 |
| 关键词 | RepSox brown adipogenesis TGF-beta receptor TGF-beta inhibitor adipocyte differentiation |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/s41401-019-0264-2 |
| 通讯作者 | Xie, Xin(xxie@simm.ac.cn) |
| 英文摘要 | Unlike white adipose tissue (WAT), brown adipose tissue (BAT) is mainly responsible for energy expenditure via thermogenesis by uncoupling the respiratory chain. Promoting the differentiation of brown fat precursor cells and the browning of white fat have become a research hotspot for the treatment of obesity and associated metabolic diseases. Several secreted factors and a number of small molecules have been found to promote brown adipogenesis. Here we report that a single small-molecule compound, RepSox, is sufficient to induce adipogenesis from mouse embryonic fibroblasts (MEFs) in fibroblast culture medium. RepSox is an inhibitor of the transforming growth factor-beta receptor I (TGF-beta-RI), other inhibitors of TGF-beta pathway such as SB431542, LY2157299, A83-01, and Tranilast are also effective in inducing adipogenesis from MEFs. These adipocytes express brown adipocyte-specific transcription factors and thermogenesis genes, and contain a large number of mitochondria and have a high level of mitochondrial respiratory activity. More interestingly, RepSox has also been found to promote the differentiation of the brown fat precursor cells and induce browning of the white fat precursor cells. These findings suggest that inhibitors of TGF-beta signaling pathway might be developed as new therapeutics for obesity and type 2 diabetes. |
| WOS关键词 | ADIPOSE-TISSUE ; FAT DEVELOPMENT ; CONVERSION ; DIFFERENTIATION ; THERMOGENESIS ; OBESITY |
| 资助项目 | Ministry of Science and Technology of China[2015CB964503] ; Ministry of Science and Technology of China[2017YFA0104002] ; Chinese Academy of Sciences[XDA16010202] ; National Natural Science Foundation of China[81425024] ; National Natural Science Foundation of China[81730099] ; National Natural Science Foundation of China[81472862] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000500546400003 |
| 出版者 | NATURE PUBLISHING GROUP |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/281995]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Xie, Xin |
| 作者单位 | 1.Tongji Univ, Shanghai Key Lab Signaling & Dis Res, Sch Life Sci & Technol, Lab Receptor Based Biomed, Shanghai 200092, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China |
| 推荐引用方式 GB/T 7714 | Tu, Wan-zhi,Fu, Yan-bin,Xie, Xin. RepSox, a small molecule inhibitor of the TGF beta receptor, induces brown adipogenesis and browning of white adipocytes[J]. ACTA PHARMACOLOGICA SINICA,2019,40(12):1523-1531. |
| APA | Tu, Wan-zhi,Fu, Yan-bin,&Xie, Xin.(2019).RepSox, a small molecule inhibitor of the TGF beta receptor, induces brown adipogenesis and browning of white adipocytes.ACTA PHARMACOLOGICA SINICA,40(12),1523-1531. |
| MLA | Tu, Wan-zhi,et al."RepSox, a small molecule inhibitor of the TGF beta receptor, induces brown adipogenesis and browning of white adipocytes".ACTA PHARMACOLOGICA SINICA 40.12(2019):1523-1531. |
入库方式： OAI收割
来源：上海药物研究所
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