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- W3011032013 abstract "Glutathionetransferase omega-1 (GSTO1-1) is an enzyme whosefunction supports the activation of interleukin (IL)-1β andIL-18 that are implicated in a variety of inflammatory disease statesfor which small-molecule inhibitors are sought. The potent reactivityof the active-site cysteine has resulted in reported inhibitors thatact by covalent labeling. In this study, structure–activityrelationship (SAR) elaboration of the reported GSTO1-1 inhibitor C1-27 was undertaken. Compounds were evaluated for inhibitoryactivity toward purified recombinant GSTO1-1 and for indicators oftarget engagement in cell-based assays. As covalent inhibitors, the kinact/KI valuesof selected compounds were determined, as well as in vivo pharmacokineticsanalysis. Cocrystal structures of key novel compounds in complex withGSTO1-1 were also solved. This study represents the first applicationof a biochemical assay for GSTO1-1 to determine kinact/KI values for testedinhibitors and the most extensive set of cell-based data for a GSTO1-1inhibitor SAR series reported to date. Our research culminated inthe discovery of 25, which we propose as the preferredbiochemical tool to interrogate cellular responses to GSTO1-1 inhibition." @default.
- W3011032013 created "2020-03-23" @default.
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- W3011032013 date "2020-02-27" @default.
- W3011032013 modified "2023-09-23" @default.
- W3011032013 title "Development ofBenzenesulfonamide Derivatives as PotentGlutathione Transferase Omega‑1 Inhibitors" @default.
- W3011032013 doi "https://doi.org/10.1021/acs.jmedchem.9b01391.s001" @default.
- W3011032013 hasPublicationYear "2020" @default.
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