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
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Research Support, Non-U.S. Gov't
MeSH terms
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Cystathionine beta-Synthase / antagonists & inhibitors*
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Cystathionine beta-Synthase / metabolism
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Cystathionine gamma-Lyase / antagonists & inhibitors*
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Cystathionine gamma-Lyase / metabolism
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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High-Throughput Screening Assays*
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Hydrogen Sulfide / antagonists & inhibitors*
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Hydrogen Sulfide / metabolism
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Signal Transduction / drug effects*
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Cystathionine beta-Synthase
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Cystathionine gamma-Lyase
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Hydrogen Sulfide