title: High-throughput tandem-microwell assay identifies inhibitors of the hydrogen sulfide signaling pathway.
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.
authors.affiliation: Key Laboratory of Systems Biomedicine (Ministry of Education), Shanghai Center for Systems Biomedicine, Shanghai Jiao Tong University, Shanghai, 200240, China. fang.wu@sjtu.edu.cn.
authors.forename: Yueyang
authors.initials: Y
authors.lastname: Zhou
authors.forename: Jing
authors.initials: J
authors.lastname: Yu
authors.forename: Xiling
authors.initials: X
authors.lastname: Lei
authors.forename: Jianying
authors.initials: J
authors.lastname: Wu
authors.forename: Qi
authors.initials: Q
authors.lastname: Niu
authors.forename: Yixuan
authors.initials: Y
authors.lastname: Zhang
authors.forename: Hong
authors.initials: H
authors.lastname: Liu
authors.forename: Philipp
authors.initials: P
authors.lastname: Christen
authors.forename: Heinz
authors.initials: H
authors.lastname: Gehring
authors.forename: Fang
authors.initials: F
authors.lastname: Wu
mesh_terms: D003541:Cystathionine beta-Synthase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D003542:Cystathionine gamma-Lyase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D057166:High-Throughput Screening Assays; D006862:Hydrogen Sulfide / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D003541:Cystathionine beta-Synthase; D003542:Cystathionine gamma-Lyase; D006862:Hydrogen Sulfide