Applied Biological Chemistry

The Korean Society for Applied Biological Chemistry (한국응용생명화학회)
권호 표지

Inhibition of Aminopeptidase N by 2-Hydroxy-3-amino-4-(p-nitrophenyl)butyryl Peptide Derivatives

  • Chung, Myung-Chul (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology) ;
  • Lee, Choong-Hwan (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology) ;
  • Lee, Ho-Jae (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology) ;
  • Chun, Hyo-Kon (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology) ;
  • Kho, Yung-Hee (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology)
  • Published : 1998.12.31
Download PDF
⟨ Previous Next ⟩

Abstract

To investigate the inhibitory activity of 2-hydroxy-3-amino-4-phenylbutyrate-harboring aminopeptidase N inhibitors, p-nitro-AHPA-peptide derivatives (1 and 2) and an AHPA-peptide derivative (3) were synthesized by chain elongation from C-terminal end using DCC/HOBt as a coupling reagent. The peptides $1{\sim}3$ exerted strong inhibitory activities against aminopeptidase N with $IC_{50}$ values of 1.8, 7.3 and $24.0\;{\mu}g/ml$, respectively, and cytotoxicity on cancer cell lines in vitro.

Keywords