Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine γ‑Lyase

Hu, Youtian; Wang, Lu; Han, Xu; Zhou, Yueyang; Zhang, Tonghui; Wang, Li; Hong, Ting; Zhang, Wei; Guo, Xun-Xiang; Sun, Jielin; Qi, Yingxin; Yu, Jing; Liu, Hong; Wu, Fang;
  • Publisher: Figshare
  • Related identifiers: doi: 10.1021/acs.jmedchem.8b01720.s003, doi: 10.1021/acs.jmedchem.8b01720.s002
  • Subject: rescues hypotension | Bioactive Inhibitor | NSC 4056 | H 2 S-generating enzyme | submicromolar inhibitors | Tyr residues | IC 50 | Pharmacology | CSE activity | 0.6 μ M | tandem-well-based high-throughput assay | chemical scaffolds | Microbiology | cystathionine γ- lyase | cystathionine β- synthase | New Scaffold | CBS | Biochemistry | Cancer | aurintricarboxylic acid | hemorrhagic shock rats
    • FOR: 59999 Environmental Sciences not elsewhere classified | 69999 Biological Sciences not elsewhere classified | 39999 Chemical Sciences not elsewhere classified
    mesheuropmc: parasitic diseases

We identify three submicromolar inhibitors with new chemical scaffolds for cystathionine γ-lyase (CSE) by a tandem-well-based high-throughput assay. NSC4056, the most potent inhibitor with an IC<sub>50</sub> of 0.6 μM, which is also known as aurintricarboxyl... View more
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