synthesisandlarinhibitionof7alkoxyanaloguesofilludalicacid
文献类型：期刊论文
| 作者 | Zhou Yueyang1; Cai Zhengliang2; Zhang Yahui1; Xiong Bing2 ; Ma Lanping2; Wang Xin2; Li Xin2; Li Jia1; Shen Jingkang2; Ling Qing2
|
| 刊名 | 药学学报
 |
| 出版日期 | 2010 |
| 卷号 | 45期号:11页码:1385 |
| 关键词 | 人源白细胞共同抗原相关蛋白 illudalic酸 抑制剂 类似物 构效关系 |
| ISSN号 | 0513-4870 |
| 英文摘要 | To obtain higher potency and specificity,a series of 7-alkoxy analogues of illudalic acid was synthesized on the base of structure-activity relationship(SAR).All of these compounds exhibited submicromolar inhibition of the enzyme when tested against human leukocyte common antigen-related phosphatase(LAR)(for example, for 15e,IC50 = 180 nmol. L-1). They represent the most potent small-molecule inhibitors of LAR so far. These analogues also display excellent selectivity for LAR over other protein tyrosine phosphatases(PTPs) except for the highly homologous PTPσ.The compound 15f is of 120-fold selectivity for LAR versus PTP-1B inhibition. The development of potent enzyme-specific inhibitors is so important that they may serve both as tools to study the role of LAR and as therapeutic agents for treatment of type II diabetes |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/286314]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.National Center for Drug Screening 2.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Zhou Yueyang,Cai Zhengliang,Zhang Yahui,et al. synthesisandlarinhibitionof7alkoxyanaloguesofilludalicacid[J]. 药学学报,2010,45(11):1385. |
| APA | Zhou Yueyang.,Cai Zhengliang.,Zhang Yahui.,Xiong Bing.,Ma Lanping.,...&Ling Qing.(2010).synthesisandlarinhibitionof7alkoxyanaloguesofilludalicacid.药学学报,45(11),1385. |
| MLA | Zhou Yueyang,et al."synthesisandlarinhibitionof7alkoxyanaloguesofilludalicacid".药学学报 45.11(2010):1385. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。