Description
4E1RCat is an inhibitor of the eIF4F translation initiation complex that blocks eIF4E:eIF4G and eIF4E:4E-BP1 interactions. It has been shown to prevent the assembly of the eIF4F complex and to inhibit cap-dependent translation with an IC
50 value of ~4 μM. 4E1RCat was shown to reverse tumor chemoresistance in a mouse model of lymphoma by sensitizing cells to the proapoptotic action of DNA damage.
Uses
4E1RCat was used to inhibit new protein synthesis in transformed primary chicken embryo fibroblasts.
Biochem/physiol Actions
4E1RCat ilnhibits the eIF4F translation initiation complex by binding to IF4E b and inhibiting the interaction between IF4E:eIF4G (IC50 = 3.2 μM). In in vitro translation experiments using MDA-MB-231 cells, 4E1RCat dose dependently inhibited cap-dependent translation, led to a decrease in polysome and 80S ribosomal subunits and reduced levels of the eIF4F-dependant proteins Mcl-1 and c-Myc.
