OF4949, NEW INHIBITORS OF AMINOPEPTIDASE B IV. EFFECTS OF OF4949 AND ITS DERIVATIVES ON ENZYME SYSTEMS

SUSUMU SANO; KATSUSHIGE IKAI; YOSHIE YOSHIKAWA; TERUYA NAKAMURA; AKIRA OBAYASHI

doi:10.7164/antibiotics.40.512

The Journal of Antibiotics

Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820

OF4949, NEW INHIBITORS OF AMINOPEPTIDASE B

IV. EFFECTS OF OF4949 AND ITS DERIVATIVES ON ENZYME SYSTEMS

SUSUMU SANO, KATSUSHIGE IKAI, YOSHIE YOSHIKAWA, TERUYA NAKAMURA, AKIRA OBAYASHI

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JOURNAL FREE ACCESS

1987 Volume 40 Issue 4 Pages 512-518

DOI https://doi.org/10.7164/antibiotics.40.512

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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-β-naphthylamide was 8×10^-9M. 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.

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