Sclerotiamide: The First Non-Peptide-Based Natural Product Activator of Bacterial Caseinolytic Protease P

J Nat Prod. 2016 Apr 22;79(4):1193-7. doi: 10.1021/acs.jnatprod.5b01091. Epub 2016 Mar 11.

Abstract

Caseinolytic protease P (ClpP) maintains essential roles in bacterial homeostasis. As such, both the inhibition and activation of this enzyme result in bactericidal activity, making ClpP a promising target for antibacterial drug development. Herein, we report the results of a fluorescence-based screen of ∼450 structurally diverse fungal and bacterial secondary metabolites. Sclerotiamide (1), a paraherquamide-related indolinone, was identified as the first non-peptide-based natural product activator of ClpP. Structure-activity relationships arising from the initial screen, preliminary biochemical evaluation of 1, and rationale for the exploitation of this chemotype to develop novel ClpP activators are presented.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Biological Products / chemistry*
  • Biological Products / pharmacology*
  • Catalysis
  • Endopeptidases / metabolism*
  • Indolizines / chemistry*
  • Indolizines / pharmacology*
  • Molecular Structure
  • Nuclear Magnetic Resonance, Biomolecular
  • Protein Conformation
  • Spiro Compounds / chemistry*
  • Spiro Compounds / pharmacology*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Biological Products
  • Indolizines
  • Spiro Compounds
  • sclerotiamide
  • Endopeptidases
  • paraherquamide