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

Phalguni Ghosh, Chunkyung Park, Mark S. Peterson, Peter B. Bitterman, Vitaly A. Polunovsky, Carston R. Wagner

Research output: Contribution to journalArticle

30 Scopus citations

Abstract

Cap-dependent translation is initiated by the binding of eIF4E to capped mRNA (m7GpppN). 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.

Original languageEnglish (US)
Pages (from-to)2177-2180
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number8
DOIs
StatePublished - Apr 15 2005

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