Novel propeptin analog, propeptin-2, missing two amino acid residues from the propeptin C-terminus loses antibiotic potency

J Antibiot (Tokyo). 2007 Aug;60(8):519-23. doi: 10.1038/ja.2007.66.

Abstract

A novel inhibitor of prolyl endopeptidase, the propeptin analog propeptin-2 (C105H130N24O(24)), missing two amino acid residues from the propeptin C-terminus was isolated from the fermentation broth of propeptin-producing Microbispora sp. SNA-115 grown using a large inoculum. It shows the same enzyme inhibition activity as propeptin against prolyl endopeptidase (Ki=1.5 microM), but its antimicrobial activity against Mycobacterium phlei is more than 100-fold lower.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actinomycetales / growth & development
  • Actinomycetales / metabolism*
  • Amino Acids / metabolism
  • Culture Media / metabolism
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Microbial Sensitivity Tests
  • Mycobacterium phlei / drug effects
  • Peptides, Cyclic / chemistry*
  • Peptides, Cyclic / metabolism*
  • Peptides, Cyclic / pharmacology
  • Prolyl Oligopeptidases
  • Serine Endopeptidases / metabolism
  • Structure-Activity Relationship

Substances

  • Amino Acids
  • Culture Media
  • Enzyme Inhibitors
  • Peptides, Cyclic
  • propeptin
  • Serine Endopeptidases
  • Prolyl Oligopeptidases