The Novel Synthetic Substance MR-387C[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-valyl-L-prolyl-L-leucine] as an Aminopeptidase M Inhibitor

  • Chung, Myung-Chul (Microbial Chemistry Research Group, Genetic Engineering Research Institute Korea Institute of Science and Technology) ;
  • Chun, Hyo-Kon (Microbial Chemistry Research Group, Genetic Engineering Research Institute Korea Institute of Science and Technology) ;
  • Lee, Ho-Jae (Microbial Chemistry Research Group, Genetic Engineering Research Institute Korea Institute of Science and Technology) ;
  • Kho, Yung-Hee (Microbial Chemistry Research Group, Genetic Engineering Research Institute Korea Institute of Science and Technology)
  • Received : 0
  • Accepted : 0
  • Published : 0

Abstract

In the course of screening for new aminopeptidase M inhibitors which were expected to be analgesic, immunopotentiating, or anti-metastatic agents, the novel synthetic substance MR-387C[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-valyl-L-prolyl-L-leucine] (M.W. 504 daltons) was obtained. It was competitive with the substrate and had an $IC_{50}$ value of $0.04\;{\mu}m/ml$ ($7.9{\times}10^{-8}\;M$) and an inhibition constant ($K_i$) of $3.8{\times}10^{-8}\;M$. This novel MR-387C was compared with various known inhibitors of aminopeptidase M. It inhibited the enzyme more strongly than any other microorganism-originated inhibitor, except probestin.

Keywords

Aminopeptidase M;inhibitor;synthetic peptide