氨肽酶B的新型抑制剂OF4949。IV. OF4949及其衍生物对酶系统的影响。

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

作者信息

Sano S, Ikai K, Yoshikawa Y, Nakamura T, Obayashi A

出版信息

J Antibiot (Tokyo). 1987 Apr;40(4):512-8. doi: 10.7164/antibiotics.40.512.

DOI:10.7164/antibiotics.40.512

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 X 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 inhibitory effects of various derivatives of I and II on aminopeptidase B activity, showed that the terminal amino and carboxamide groups are essential for activity.

摘要

OF4949-I和II以竞争性方式抑制艾氏腹水癌细胞的氨肽酶B，二者对L-精氨酸-β-萘酰胺的Ki值均为8×10⁻⁹ M。检测了I和II对各种外肽酶和内肽酶的抑制作用。OF4949-I和II均强烈抑制亮氨酸氨肽酶和脑啡肽降解氨肽酶；I还抑制脑啡肽酶B。I和II的各种衍生物对氨肽酶B活性的抑制作用表明，末端氨基和羧酰胺基团对活性至关重要。