中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
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

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