A practical fluorogenic substrate for high-throughput screening of glutathione S-transferase inhibitors

Chem Commun (Camb). 2015 Jul 21;51(57):11459-62. doi: 10.1039/c5cc02067k.

Abstract

We report a new fluorogenic substrate for glutathione S-transferase (GST), 3,4-DNADCF, enabling the assay with a low level of nonenzymatic background reaction. Inhibitors against Noppera-bo/GSTe14 from Drosophila melanogaster were identified by high throughput screening using 3,4-DNADCF, demonstrating the utility of this substrate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drosophila Proteins / antagonists & inhibitors*
  • Drosophila Proteins / metabolism
  • Drosophila melanogaster / enzymology*
  • Drug Evaluation, Preclinical
  • Enzyme Assays
  • Enzyme Inhibitors / pharmacology*
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / metabolism*
  • Glutathione / chemistry
  • Glutathione / metabolism
  • Glutathione Transferase / antagonists & inhibitors*
  • Glutathione Transferase / metabolism
  • High-Throughput Screening Assays
  • Humans
  • Spectrometry, Fluorescence
  • Substrate Specificity

Substances

  • Drosophila Proteins
  • Enzyme Inhibitors
  • Fluorescent Dyes
  • Glutathione Transferase
  • Gste14 protein, Drosophila
  • Glutathione