Illudalic acid as a potential LAR inhibitor: Synthesis, SAR, and preliminary studies on the mechanism of action
文献类型：期刊论文
| 作者 | Ling, Qing2; Huang, Yue2; Zhou, Yueyang1; Cai, Zhengliang2; Xiong, Bing2 ; Zhang, Yahui1; Ma, Lanping2; Wang, Xin2; Li, Xin2; Li, Jia1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2008-08-01 |
| 卷号 | 16期号:15页码:7399-7409 |
| 关键词 | human leukocyte common antigen-related phosphatase (LAR) illudalic acid inhibitor mechanism structure-activity relationship (SAR) synthesis |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2008.06.014 |
| 文献子类 | Article |
| 英文摘要 | A novel synthesis of the human leukocyte common antigen-related (LAR) phosphatase inhibitor, illudalic acid, has been achieved by a route more amenable to structure modi. cations. A series of simpler analogues of illudalic acid was synthesized and evaluated for potency in inhibiting LAR. The structure -activity relationship (SAR) study has shown that the 5-formyl group and the hemi-acetal lactone are crucial for effective inhibition of LAR activity, and are the key pharmacophores of illudalic acid. The fused dimethylcyclopentene ring moiety evidently helps to enhance the potency of illudalic acid against LAR. A preliminary study of the mechanism of action of illudalic acid against LAR was conducted using electrospray ionization mass spectrometry (ESI-MS) and molecular docking techniques. The results are in full agreement with the described mechanism. (C) 2008 Elsevier Ltd. All rights reserved. |
| WOS关键词 | PROTEIN-TYROSINE PHOSPHATASES ; LEUKOCYTE-COMMON ANTIGEN ; STRUCTURE-BASED DESIGN ; 1B INHIBITORS ; ALLOSTERIC-INHIBITION ; MASS-SPECTROMETRY ; PTP1B INHIBITORS ; INSULIN-RECEPTOR ; DISCOVERY ; BETA |
| 资助项目 | Hi-Tech Research and Development Program of China[2006AA02Z315] ; Hi-tech Research and Development Program of China[2007AA09Z402] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000258749500034 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272847]  |
| 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 药物化学研究室 |
| 通讯作者 | Li, Jia |
| 作者单位 | 1.Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ling, Qing,Huang, Yue,Zhou, Yueyang,et al. Illudalic acid as a potential LAR inhibitor: Synthesis, SAR, and preliminary studies on the mechanism of action[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(15):7399-7409. |
| APA | Ling, Qing.,Huang, Yue.,Zhou, Yueyang.,Cai, Zhengliang.,Xiong, Bing.,...&Shen, Jingkang.(2008).Illudalic acid as a potential LAR inhibitor: Synthesis, SAR, and preliminary studies on the mechanism of action.BIOORGANIC & MEDICINAL CHEMISTRY,16(15),7399-7409. |
| MLA | Ling, Qing,et al."Illudalic acid as a potential LAR inhibitor: Synthesis, SAR, and preliminary studies on the mechanism of action".BIOORGANIC & MEDICINAL CHEMISTRY 16.15(2008):7399-7409. |
入库方式： OAI收割
来源：上海药物研究所
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