L-leucinthiol - a potent inhibitor of leucine aminopeptidase

Abstract

L-leucinthiol (2-amino-4-methyl-1-pentanethiol) was designed as an inhibitor of leucine aminopeptidase by analogy with sulfhydryl inhibitors of other zinc-containing peptidases. It was synthesized from L-leucinol and shown to be a potent competitive inhibitor of the microsomal aminopeptidase from porcine kidney (Ki = 2.2 X 10(-8) M). The results suggest that the mechanism of aminopeptidase may be similar to that of other metalloproteases.