Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein
文献类型：期刊论文
| 作者 | Wang, Tianlu2; Hong, Tingting2; Huang, Yue1; Su, Haomiao2; Wu, Fan2; Chen, Yi2 ; Wei, Lai2; Huang, Wei2; Hua, Xiaoluan2; Xia, Yu2
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| 刊名 | JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
 |
| 出版日期 | 2015-11-04 |
| 卷号 | 137期号:43页码:13736-13739 |
| ISSN号 | 0002-7863 |
| DOI | 10.1021/jacs.5b06690 |
| 文献子类 | Article |
| 英文摘要 | The FTO protein is unequivocally reported to play a critical role in human obesity and in the regulation of cellular levels of m(6)A modification, which makes FTO a significant and worthy subject of study. Here, we identified that fluorescein derivatives can selectively inhibit FTO demethylation, and the mechanisms behind these activities were elucidated after we determined the X-ray crystal structures of FTO/fluorescein and FTO/5-aminofluorescein. Furthermore, these inhibitors can also be applied to the direct labeling and enrichment of FTO protein combined with photoaffinity labeling assay. |
| WOS关键词 | PROMISCUOUS INHIBITORS ; RNA DEMETHYLASE ; NUCLEAR-RNA ; M(6)A ; N-6-METHYLADENOSINE ; OBESITY ; DNA ; METHYLATION ; ALKBH5 ; N6-METHYLADENOSINE |
| 资助项目 | 973 Program[2012CB720600] ; 973 Program[2012CB720603] ; 973 Program[2012CB720604] ; 973 Program[2015CB910603] ; National Science Foundation of China[21432008] ; National Science Foundation of China[91413109] ; National Science Foundation of China[91213302] ; National Science Foundation of China[21372237] ; National Science Foundation of China[91313303] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000364355900004 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276332]  |
| 专题 | 药理学第三研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Zhou, Xiang |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Medica, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Wuhan Univ, Coll Chem & Mol Sci, Inst Adv Studies & Sch Med, Wuhan 430072, Hunan, Peoples R China; 3.Fudan Univ, Sch Life Sci, Shanghai 200433, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Tianlu,Hong, Tingting,Huang, Yue,et al. Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2015,137(43):13736-13739. |
| APA | Wang, Tianlu.,Hong, Tingting.,Huang, Yue.,Su, Haomiao.,Wu, Fan.,...&Zhou, Xiang.(2015).Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein.JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,137(43),13736-13739. |
| MLA | Wang, Tianlu,et al."Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein".JOURNAL OF THE AMERICAN CHEMICAL SOCIETY 137.43(2015):13736-13739. |
入库方式： OAI收割
来源：上海药物研究所
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