文献类型：期刊文献

英文题名：Discovering the distinct inhibitory effects between C4-epimeric glycosyl amino acids: new insight into the development of protein tyrosine phosphatase inhibitors

作者：He, Xiao-Peng[1,2,3,5];Li, Cui[1,2,3];Wang, Zhi-Zhou[1,2,3];Gao, Li-Xin[1,2,3];Shi, Xiao-Xin[1,2,3];Tang, Yun[1,2,3];Xie, Juan[5];Li, Jia[4];Chen, Guo-Rong[1,2,3];Chen, Kaixian[1,2,3,4]

机构：[1]E China Univ Sci & Technol, Key Lab Adv Mat, Shanghai 200237, Peoples R China;[2]E China Univ Sci & Technol, Inst Fine Chem, Shanghai 200237, Peoples R China;[3]E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China;[4]Chinese Acad Sci, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, State Key Lab Drug Res,Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;[5]CNRS, PPSM, Inst Alembert, ENS Cachan,UMR 8531, F-94235 Cachan, France

年份：2011

卷号：28

期号：7

起止页码：493

外文期刊名：GLYCOCONJUGATE JOURNAL

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000297745200007)】；

基金：Project supported by National Natural Science Foundation of China (Grant No. 20876045, No. 30801405), National Basic Research Program of China (No. 2007CB914201), Shanghai Science and Technology Community (No. 10410702700), Chinese Academy of Sciences (No. KSCX2-EW-R-15) and the Fundamental Research Funds for the Central Universities (No. WK1013002). X.-P. He also gratefully acknowledges the French Embassy in PR China for a co-tutored doctoral fellowship.

语种：英文

外文关键词：Epimer; Sugar template; PTP inhibitor; Click chemistry; Molecular docking study

摘要：There has been increasing interest in the development of drug candidates based on sugar templates that possess rich structural and, especially, configurational diversities. We disclose herein that the epimeric identity between methyl 3,4-bis-phenylalanyl/tyrosinyl triazolyl-alpha-D-galactopyranoside and glucopyranoside may lead to their distinct inhibitory effects on specific protein tyrosine phosphatases (PTPs). Subsequently performed molecular docking study elucidated the plausible binding behaviors of the more potent galactosyl inhibitors with their primary PTP target, i.e. Cell Division Cycle 25B (CDC25B) phosphatase.