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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Wenfang Xu

Volume 6, Issue 6, 2009

Page: [420 - 423] Pages: 4

DOI: 10.2174/157018009789057535

Price: $65

Abstract

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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