High-throughput tandem-microwell assay identifies inhibitors of the hydrogen sulfide signaling pathway

Chem Commun (Camb). 2013 Dec 28;49(100):11782-4. doi: 10.1039/c3cc46719h.

Abstract

We report a high-throughput assay for H2S-producing enzymes, which is based on a newly designed tandem-well plate. Screening of 21,599 agents identified several potent inhibitors of cystathionine β-synthase and cystathionine γ-lyase, the two key enzymes generating H2S in mammals, with IC50 values in the low two-digit micromolar range.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cystathionine beta-Synthase / antagonists & inhibitors*
  • Cystathionine beta-Synthase / metabolism
  • Cystathionine gamma-Lyase / antagonists & inhibitors*
  • Cystathionine gamma-Lyase / metabolism
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • High-Throughput Screening Assays*
  • Hydrogen Sulfide / antagonists & inhibitors*
  • Hydrogen Sulfide / metabolism
  • Signal Transduction / drug effects*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Cystathionine beta-Synthase
  • Cystathionine gamma-Lyase
  • Hydrogen Sulfide