%0 Generic
%A Hu, Youtian
%A Wang, Lu
%A Han, Xu
%A Zhou, Yueyang
%A Zhang, Tonghui
%A Wang, Li
%A Hong, Ting
%A Zhang, Wei
%A Guo, Xun-Xiang
%A Sun, Jielin
%A Qi, Yingxin
%A Yu, Jing
%A Liu, Hong
%A Wu, Fang
%D 2018
%T Discovery of a
Bioactive Inhibitor with a New Scaffold
for Cystathionine γ‑Lyase
%U https://acs.figshare.com/articles/dataset/Discovery_of_a_Bioactive_Inhibitor_with_a_New_Scaffold_for_Cystathionine_Lyase/7533248
%R 10.1021/acs.jmedchem.8b01720.s003
%2 https://ndownloader.figshare.com/files/14005496
%K 0.6 μ M
%K IC 50
%K NSC 4056
%K cystathionine β- synthase
%K tandem-well-based high-throughput assay
%K chemical scaffolds
%K Tyr residues
%K hemorrhagic shock rats
%K submicromolar inhibitors
%K rescues hypotension
%K CSE activity
%K cystathionine γ- lyase
%K Bioactive Inhibitor
%K aurintricarboxylic acid
%K H 2 S-generating enzyme
%K New Scaffold
%K CBS
%X 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 IC50 of
0.6 μM, which is also known as aurintricarboxylic acid, selectively
binds to Arg and Tyr residues of CSE active site and preferably inhibits
the CSE activity in cells rather than cystathionine β-synthase
(CBS), the other H2S-generating enzyme. Moreover, NSC4056
effectively rescues hypotension in hemorrhagic shock rats.
%I ACS Publications