Total synthesis of grassystatin A, a probe for cathepsin E function

Bioorg Med Chem. 2012 Aug 1;20(15):4774-80. doi: 10.1016/j.bmc.2012.05.077. Epub 2012 Jun 7.

Abstract

The linear depsipeptide grassystatin A, a valuable probe for the study of cathepsin E function, has been synthesized by a [4+6] strategy. It exhibited specific inhibitory activity against cathepsin E with an IC(50) value of 0.8 nM. Our studies indicated that inhibition of cathepsin E did not have an impact on ovalbumin antigen processing and peptide presentation, unique from studies of other aspartic protease inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cathepsin E / antagonists & inhibitors*
  • Cathepsin E / metabolism
  • Dose-Response Relationship, Drug
  • Female
  • Male
  • Mice
  • Mice, Transgenic
  • Molecular Structure
  • Peptides / chemical synthesis
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Protease Inhibitors / chemical synthesis
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Peptides
  • Protease Inhibitors
  • grassystatin A
  • Cathepsin E