Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C
文献类型：期刊论文
| 作者 | Li Dan1; Yin Jianpeng2; Li Jingya2 ; Nan Fajun2
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2016-06-25 |
| 卷号 | 36期号:6页码:1359-1367 |
| 关键词 | aphadilactone C DGAT1 selective inhibitor PF-04620110 AZD-7687 |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201511037 |
| 文献子类 | Article |
| 英文摘要 | Diacylglycerol acyltransferase (DGAT), the only limited enzyme in the synthesis of triacylglycerol (TAG), is regarded as an important therapeutic target for human obesity and other metabolic syndromes. Compounds 5 similar to 8 were designed and synthesized, in which the lactone group of aphadilactone C was introduced into the PF-04620110 and AZD-7687, which have entered into the clinical research, to verify whether the lactone in aphadilactone C played the same role as carboxylic group in PF-04620110 and AZD-7687. The final vitro assay showed that compounds 5 similar to 8 have not the inhibition activity to DGAT1. This might suggest that inhibition mechanism of aphadilactone C was not the same as PF-04620110 and AZD-7687. |
| WOS关键词 | TRIGLYCERIDE SYNTHESIS ; OBESITY RESISTANCE ; MICE ; DISCOVERY ; CLONING ; POTENT ; FAMILY ; DGAT2 |
| 资助项目 | Shanghai Key Laboratory of Psychotic Disorders[13DZ226050014K-10] |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5748046 |
| WOS记录号 | WOS:000384603800018 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275985]  |
| 专题 | 国家新药筛选中心 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 | Nan Fajun |
| 作者单位 | 1.East China Normal Univ, Coll Chem & Mol Engn, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li Dan,Yin Jianpeng,Li Jingya,et al. Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2016,36(6):1359-1367. |
| APA | Li Dan,Yin Jianpeng,Li Jingya,&Nan Fajun.(2016).Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C.CHINESE JOURNAL OF ORGANIC CHEMISTRY,36(6),1359-1367. |
| MLA | Li Dan,et al."Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C".CHINESE JOURNAL OF ORGANIC CHEMISTRY 36.6(2016):1359-1367. |
入库方式： OAI收割
来源：上海药物研究所
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