Design and synthesis of Atglistatin derivatives as adipose triglyceride lipase inhibitors
文献类型：期刊论文
| 作者 | Jin, Jiyu1; Huang, Suling2 ; Wang, Lei1; Leng, Ying2; Lu, Wei1
|
| 刊名 | CHEMICAL BIOLOGY & DRUG DESIGN
 |
| 出版日期 | 2017-12 |
| 卷号 | 90期号:6页码:1122-1133 |
| 关键词 | adipose triglyceride lipase inhibitors Atglistatin structure-activity relationship thiourea |
| ISSN号 | 1747-0277 |
| DOI | 10.1111/cbdd.13029 |
| 文献子类 | Article |
| 英文摘要 | Adipose triglyceride lipase (ATGL) is a rate-limiting enzyme that mobilizes fatty acids from cellular triglyceride stores. Metabolic syndrome, which refers to a group of abnormalities that occur together and increase the risk of coronary artery disease, stroke, type 2 diabetes, and cachexia, can be treated using ATGL-specific inhibitors. Atglistatin (1) is the first small-molecule inhibitor of ATGL. In this study, we designed and synthesized 29 Atglistatin derivatives and evaluated their inhibition of forskolin-stimulated lipolysis in 3T3-L1 adipocytes as an indicator of their potential to inhibit ATGL in adipose tissues. Among all the tested Atglistatin analogs, we previously found that the thiourea compound 9e showed potent ATGL inhibitory activity in vitro, which was much stronger than that of Atglistatin, and its inhibitory activity in vivo was similar to that of Atglistatin. This tool compound could be used to study the pathophysiology and druggability of ATGL in animal models of metabolic disease and cachexia. |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000415354300008 |
| 出版者 | WILEY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272387]  |
| 专题 | 药理学第一研究室 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 | Leng, Ying; Lu, Wei |
| 作者单位 | 1.East China Normal Univ, Sch Chem & Mol Engn, Shanghai, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jin, Jiyu,Huang, Suling,Wang, Lei,et al. Design and synthesis of Atglistatin derivatives as adipose triglyceride lipase inhibitors[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2017,90(6):1122-1133. |
| APA | Jin, Jiyu,Huang, Suling,Wang, Lei,Leng, Ying,&Lu, Wei.(2017).Design and synthesis of Atglistatin derivatives as adipose triglyceride lipase inhibitors.CHEMICAL BIOLOGY & DRUG DESIGN,90(6),1122-1133. |
| MLA | Jin, Jiyu,et al."Design and synthesis of Atglistatin derivatives as adipose triglyceride lipase inhibitors".CHEMICAL BIOLOGY & DRUG DESIGN 90.6(2017):1122-1133. |
入库方式： OAI收割
来源：上海药物研究所
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