OF4949, new inhibitors of aminopeptidase A. IV Effects of OF4949 and its derivatives on enzyme systems.

Publisher Website
Google Scholar
Abstract
OF4949-I and II inhibited aminopeptidase B from Ehrlich ascites carcinoma in a competitive way and the Ki value for both against L-arginine-.beta.-naphthylamide was 8 .times. 10-9 M. Inhibition by I and II of various exopeptidases and endopeptidases was examined. OF4949-I and II both strongly inhibited leucine aminopeptidase and enkephalin-degrading aminopeptidase; I also inhibited enkephalinase B. The inhibitor effects of various derivatives of I and II on aminopeptidase B activity, showed that the terminal amino and carboxamide groups are essential for activity.