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Pharmacy Journal

the design and synthesis of nucleotide monophosphate mimetic eIF4E inhibitors.
Fig. 1. (a) mRNA cap recognition (represented by m7GTP shown as yellow CPK sticks) and binding of eIF4G or 4E-BPs (represented by a peptide derived from 4E-BP1 shown as a
cyan cartoon) occurs on opposite faces of eIF4E (green cartoon). Apart from direct cap-binding antagonists, allosteric inhibitors (binding pose of 4-EGI1 [22] shown as magenta
sticks) and inhibitors derived from eIF4G and 4E-BPs [23] are being developed. Whereas m7GTP-binding is dominated by polar interactions between the cationic N-methylpurine
system and eIF4E residues W56, W102, and E103 (cationep interaction and H-bonds), as well as the phosphate groups with residues R157, K159, and K162,