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Activation and inhibition of leukotriene A4 hydrolase aminopeptidase activity by diphenyl ether and derivatives.

作者信息

Jiang Xiaolu, Zhou Lu, Wei Dengguo, Meng Hu, Liu Ying, Lai Luhua

机构信息

Beijing National Laboratory for Molecular Sciences, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.

出版信息

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6549-52. doi: 10.1016/j.bmcl.2008.10.044. Epub 2008 Oct 14.

Abstract

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 A(4) hydrolase.

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