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Synthesis of 7-benzylguanosine cap-analogue conjugates for eIF4E targeted degradation.

Abstract：

:Eukaryotic translation initiation factor 4E (eIF4E) is a key player in the initiation of cap-dependent translation through recognition of the m7GpppX cap at the 5' terminus of coding mRNAs. As eIF4E overexpression has been observed in a number of human diseases, most notably cancer, targeting this oncogenic translation initiation factor has emerged as a promising strategy for the development of novel anti-cancer therapeutics. Toward this end, in the present study, we have rationally designed a series of Bn7GxP-based PROTACs for the targeted degradation of eIF4E. Herein we describe our synthetic efforts, in addition to biochemical and cellular characterization of these compounds.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Kaur T,Menon A,Garner AL

doi

10.1016/j.ejmech.2019.01.080

subject

Has Abstract

pub_date

2019-03-15 00:00:00

pages

339-350

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30100-X

journal_volume

166

pub_type

杂志文章

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