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KMID : 0545119960060010007
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Journal of Microbiology and Biotechnology
1996 Volume.6 No. 1 p.7 ~ p.11
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Inhibition of Aminopeptidase N by Two Synthetic Tripeptides
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CHUNG, MYUNG-CHUL
CHUN, HYO-KON/LEE, HO-JAE/LEE, CHOONG-HWAN/KIM, SU-IL/KHO, YUNG-HEE
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Abstract
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MR-387A1 (AHPA-Val-Pro) and A2 (AHPA-Val-Hyp) were prepared as aminopeptidase N inhibitors through the synthesis of peptide MR-387A and B analugues which contained 3-amino-2-hydroxy-4-phenyl butanoic acid (AHPA) as a zinc-chelating moiety. They are competitive inhibitors of aminopeptidase N with inhibition constants (Ki) of 4.1×10^-7 and 1.1×10^-6 M, respectively. MR-387A1 also strongly inhibited aminopeptidase B of human myelogenous leukmia K-562 cell with IC_50 of 0.35 ??M. Inhibitions of aminopeptidase N activity by AHPA-bearing inhibitors of various peptide chain lengths also have been studied. IC_50 values of AHPA-Val (bestatin), AHPA-Val-Pro (MR-387A1) and AHPA-Val-Pro-Leu (MR-387C) compared against porcine kidney aminopeptidase N were 20.1, 0.60 and 0.08 ??M, respectively. These results support that a multiple interaction between the S_1→S´_3 sites of aminopeptidase N and the P_1→P´_3 of the inhibitor plays a crucial role in stabilizing strongly the enzyme-inhibitor complex.
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KEYWORD
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