The Synthesis and Activity Evaluation of a Bestatin Derivative (LYP) as an Aminopeptidase N Inhibitor

Author(s): Yepeng Luan, Xuejian Wang, Huawei Zhu, Xianjun Qu, Hao Fang, Wenfang Xu

Journal Name: Letters in Drug Design & Discovery

Volume 6 , Issue 6 , 2009

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Aminopeptidase N (APN) is a ubiquitous enzyme overexpressed on the epithelium of tumor and plays an important role in angiogenesis and metastasis of tumor. Bestatin acting as an inhibitor of Aminopeptidase N and B is used in the ancillary treatment of cancer. In this paper, we designed, synthesized a derivative of Bestatin (LYP), and evaluated the activity of it which exhibited better efficacy than Bestain in vitro and vivo.

Keywords: Aminopeptidase N, Bestatin, N, N-dimethyl ethanolamine, A549, ES-2, HL-60

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Article Details

Year: 2009
Page: [420 - 423]
Pages: 4
DOI: 10.2174/157018009789057535
Price: $65

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