Synthesis and evaluation of potential inhibitors of eIF4E cap binding to 7-methyl GTP

被引:36
|
作者
Ghosh, P
Park, C
Peterson, MS
Bitterman, PB
Polunovsky, VA
Wagner, CR [1 ]
机构
[1] Univ Minnesota, Dept Med Chem, Minneapolis, MN 55455 USA
[2] Univ Minnesota, Dept Med, Minneapolis, MN 55455 USA
关键词
D O I
10.1016/j.bmcl.2005.01.080
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Cap-dependent translation is initiated by the binding of eIF4E to capped mRNA (m(7) GpppN). We have prepared a small library of 7-methyl guanosine nucleoside and nucleotide analogs and evaluated their ability to inhibit eIF4E binding to 7-methyl GTP with a competitive eIF4E binding immunoassay. 5 '-H-Phosphonate derivatives in which the 2 '- and 3 '-riboside hydroxyls were tethered together by an isopropylidene group were shown to be a new class of inhibitors of eIF4E binding to capped mRNA. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2177 / 2180
页数:4
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