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