Inhibition of carboxypeptidase a by N-(4- t-Butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone

N-(4- t-Butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone ( 2), which is a potent inhibitor of HIV-1 reverse transcriptase, was found to inhibit carboxypeptidase A in a mixed uncompetitive-competitive mode. Molecular modeling studies suggest that 2 may inhibit CPA by binding to the S 1 and S 2 subs...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1997-06, Vol.7 (12), p.1557-1562
Main Authors: Lanthier, Christopher M., Parniak, Michael A., Dmitrienko, Gary I.
Format: Article
Language:English
Subjects:
Analytical, structural and metabolic biochemistry
Biological and medical sciences
Enzymes and enzyme inhibitors
Fundamental and applied biological sciences. Psychology
Hydrolases
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Summary:N-(4- t-Butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone ( 2), which is a potent inhibitor of HIV-1 reverse transcriptase, was found to inhibit carboxypeptidase A in a mixed uncompetitive-competitive mode. Molecular modeling studies suggest that 2 may inhibit CPA by binding to the S 1 and S 2 subsites of free CPA as well as to the CPA-phenylalanine binary enzyme-product complex. N-(4- t-Butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone ( 2), which is a potent inhibitor of HIV-1 reverse transcriptase, was found to inhibit carboxypeptidase A in a mixed uncompetitive-competitive mode. Molecular modeling studies suggest that 2 inhibits CPA by binding to the S 1 and S 2 subsites of free CPA as well as the CPA-phenylalanine binary enzyme-product complex.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)00267-9