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1. Kelatorphan and related analogs: potent and selective inhibitors of leukotriene A4 hydrolase

Author

Gwen Grabowski Krivi, E.Yvonne Pyla, Stevan W. Djuric, Thomas D. Penning, Richard A. Haack, Leslie J Askonas, Stella S. Yu, and Marshall L. Michener

Subjects
chemistry.chemical_classification, Leukotriene A4, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Peptide, Biochemistry, Aminopeptidase, Leukotriene-A4 hydrolase, chemistry.chemical_compound, Enzyme, chemistry, Drug Discovery, Hydrolase, Molecular Medicine, Kelatorphan, Molecular Biology
Abstract

The hydroxamic acid-containing peptide kelatorphan, a known inhibitor of enkephalin-degrading enzymes, is a potent, non-competitive inhibitor of leukotriene A4 (LTA4) hydrolase. Analogs of kelatorphan were prepared and several significantly and selectively inhibited both the hydrolase and aminopeptidase activity of the enzyme.

Published
1995
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