Studies on inhibition of enzymatic arginyltransfer reaction

Abstract

Synthetic polyamines and various derivatives of aspartic acid and glutamic acid were examined in vitro for their inhibitory activity on arginyl-tRNA-protein transferase. All the polyamines tested showed non- specific activation or inhibition at 0.1 or 10 mM, respectively, suggesting an interaction of polyamines with tRNA. Of the newly prepared active site directed compounds including the inhibitory peptides so far reported, L- aspartic acid α-[(S)-(-)-naphthylethylamide] was found to inhibit the enzyme activity most potently with a slight substrate activity, whereas the R- isomer showed very weak inhibition, giving information on the active site of the enzyme.