Discovery of a first-in-class inhibitor of sulfide:quinone oxidoreductase that protects against adverse cardiac remodelling and heart failure | Zendy

Michael R. Jackson | Zendy; Kristie Dawn Cox | Zendy; Simon D. P. Baugh | Zendy; Luke Wakeen | Zendy; Adel A. Rashad | Zendy; Patrick Y. S. Lam | Zendy; Boris Polyak | Zendy; Marilyn Schuman Jörns | Zendy

Open Access

Discovery of a first-in-class inhibitor of sulfide:quinone oxidoreductase that protects against adverse cardiac remodelling and heart failure

Author(s) -

Michael R. Jackson,

Kristie Dawn Cox,

Simon D. P. Baugh,

Luke Wakeen,

Adel A. Rashad,

Patrick Y. S. Lam,

Boris Polyak,

Marilyn Schuman Jörns

Publication year - 2021

Publication title -

cardiovascular research

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.774

H-Index - 219

eISSN - 1755-3245

pISSN - 0008-6363

DOI - 10.1093/cvr/cvab206

Subject(s) - heart failure , pharmacology , chemistry , medicine , biochemistry , cancer research

Hydrogen sulfide (H2S) is a potent signalling molecule that activates diverse cardioprotective pathways by post-translational modification (persulfidation) of cysteine residues in upstream protein targets. Heart failure patients with reduced ejection fraction (HFrEF) exhibit low levels of H2S. Sulfide:quinone oxidoreductase (SQOR) catalyses the first irreversible step in the metabolism of H2S and plays a key role in regulating H2S-mediated signalling. Here, the aim of this study was to discover a first-in-class inhibitor of human SQOR and evaluate its cardioprotective effect in an animal model of HFrEF.

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