LYP3, a new bestatin derivative for aminopeptidase N inhibition

Med Chem. 2011 Jan;7(1):32-6. doi: 10.2174/157340611794072706.

Abstract

Aminopeptidase N (APN) is a ubiquitous enzyme overexpressed on tumor cells and plays an important role in angiogenesis and metastasis of tumor. Bestatin as an effective inhibitor of aminopeptidase N is used for complementary treatment of cancer with other drugs. In this work, we reformed the structure of bestatin to a new derivative LYP3 to improve the water solubility and effectiveness. The inhibitory activity of LYP3 against APN was evaluated in vitro.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • CD13 Antigens / antagonists & inhibitors*
  • CD13 Antigens / chemistry
  • CD13 Antigens / metabolism
  • Cell Line, Tumor
  • Humans
  • Leucine / analogs & derivatives*
  • Leucine / chemical synthesis
  • Leucine / chemistry
  • Leucine / pharmacology
  • Matrix Metalloproteinase 2 / chemistry
  • Matrix Metalloproteinase 2 / metabolism
  • Matrix Metalloproteinase Inhibitors
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy
  • Solubility

Substances

  • LYP3 compound
  • Matrix Metalloproteinase Inhibitors
  • CD13 Antigens
  • Matrix Metalloproteinase 2
  • Leucine
  • ubenimex