Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 24, Pages 6549-6552Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.044
Keywords
Leukotriene A(4) hydrolase/aminopeptidase; Diphenyl ether derivatives; Activators; Inhibitors
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Funding
- Ministry of Science and Technology of China
- National Natural Science Foundation of China [30490245, 20773002, 20873003]
- China Postdoctoral Science Foundation [20070410433]
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The synthesis and biological evaluation of a series of diphenyl ether derivatives were described. The compounds can either activate or inhibit the aminopeptidase activity of leukotriene A(4) hydrolase, while at the same time do not influence the hydrolase activity. Further enzyme kinetics and molecular modeling investigation on these novel chemical activators revealed their possible activation mechanism. These compounds can be used as probes to regulate the aminopeptidase activity of leukotriene A4 hydrolase. (C) 2008 Elsevier Ltd. All rights reserved.
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