Design, Synthesis of Lithocholic Acid Mimics and Their Inhibitory Activities against Protein Tyrosine Phosphatase 1B
文献类型：期刊论文
| 作者 | He Haibing3; Dai Hong3; Gao Lixin1; Zhang Haijun3; Zou Zheng3; Yang Fan2; Li Jia1 ; Shi Yujun3
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2016-11 |
| 卷号 | 36期号:11页码:2670-2676 |
| 关键词 | PTP1B inhibitor steroid lithocholic acid mimics synthesis |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201605018 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase-1B (PTP1B), a negative regulatory factor of insulin signaling, is recognized as a potent target for the therapy of diabetes. Aimed to provide new scaffold to the development of PTP1B inhibitors and disclose the relationship between configurations of certain positions (3, 4, 5, 6 and 23-position) on the steroidal skeleton and inhibitory activities against PTP1B, a class of lithocholic acid (LCA) mimics were designed and synthesized. In vitro bioassay against PTP1B showed that 3,3 beta-hydroxy-4-ene-cholanic acid (17) and 4,4-dimethy1-3 beta-hydroxy-5-ene-cholanic acid (19) had activities higher than LCA, reaching (8.50 (+/-)1.21) and (6.27 +/- 1.03) mu mol.L--1,L- respectively. Docking analysis of compounds 17 and 19 illuminated the binding modes to PTP1B. This study provided compounds with new scaffold and valuable structure-activity-relationship (SAR) information for the further study of PTP1B inhibitors. |
| WOS关键词 | DIPEPTIDYL-PEPTIDASE-IV ; BIOLOGICAL EVALUATION ; INSULIN-RECEPTOR ; DERIVATIVES ; IDENTIFICATION ; DISCOVERY ; PTP1B |
| 资助项目 | Science Fund for Young Scholar of Jiangsu Province[BK20140425] ; Initiating Fund for Introduced Talents of Nantong University[03080694] |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5881758 |
| WOS记录号 | WOS:000392462300011 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275822]  |
| 专题 | 国家新药筛选中心 药物安全性评价中心 |
| 通讯作者 | Yang Fan; Shi Yujun |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Inst Mol Therapy & Med Dev MTDD, Shanghai 200062, Peoples R China 3.Nantong Univ, Coll Chem & Chem Engn, Nantong 226019, Peoples R China; |
| 推荐引用方式 GB/T 7714 | He Haibing,Dai Hong,Gao Lixin,et al. Design, Synthesis of Lithocholic Acid Mimics and Their Inhibitory Activities against Protein Tyrosine Phosphatase 1B[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2016,36(11):2670-2676. |
| APA | He Haibing.,Dai Hong.,Gao Lixin.,Zhang Haijun.,Zou Zheng.,...&Shi Yujun.(2016).Design, Synthesis of Lithocholic Acid Mimics and Their Inhibitory Activities against Protein Tyrosine Phosphatase 1B.CHINESE JOURNAL OF ORGANIC CHEMISTRY,36(11),2670-2676. |
| MLA | He Haibing,et al."Design, Synthesis of Lithocholic Acid Mimics and Their Inhibitory Activities against Protein Tyrosine Phosphatase 1B".CHINESE JOURNAL OF ORGANIC CHEMISTRY 36.11(2016):2670-2676. |
入库方式： OAI收割
来源：上海药物研究所
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