Description
In eukaryotes, a set of initiation factors (eIFs) interact with ribosomal subunits to initiate mRNA translation. A major step in initiation is the assembly of a large multiprotein complex that includes the cap-binding protein eIF4E and the multidomain adaptor protein eIF4G. 4EGI-1 is an inhibitor of the initiation of translation that blocks the interaction of eIF4G with eIF4E (K
D = 25 μM). It directly binds eIF4E, competitively inhibiting an association with eIF4G that is necessary for cap-dependent translation. 4EGI-1 prevents the expression of oncogenic proteins in mammalian cancer cells, leading to apoptosis. Research with this inhibitor supports a role for normal eIF4E/eIF4G interaction in memory consolidation and excess interaction in autism spectrum disorders. 4EGI-1 also blocks translation in some viruses that do not require eIF4E or a cap structure for initiation.
Uses
eIF4E/eIF4G Interaction Inhibitor, 4EGI-1 is amplifies TRAIL-induced apoptosis via down-regulation of FLIPS/L?and induction of DR5.
Definition
ChEBI: 4EGI-1 is a dichlorobenzene, a member of 1,3-thiazoles, a C-nitro compound, a monocarboxylic acid and a hydrazone.
References
[1] moerke n j, aktas h, chen h, et al. small-molecule inhibition of the interaction between the translation initiation factors eif4e and eif4g. cell, 2007, 128(2): 257-267.
