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- W4311779306 abstract "Sirtiun 5 (SIRT5) is a NAD+-dependent protein lysine deacylase. It is emerging as a promising target for the development of drugs to treat cancer and metabolism-related diseases. In this study, we screened 5000 compounds and identified a hit compound 14 bearing a pyrazolone functional group as a novel SIRT5-selective inhibitor. Structure-based optimization of 14 resulted in compound 47 with an IC50 value of 0.21 ± 0.02 μM and a 100-fold improved potency. Compound 47 showed substantial selectivity for SIRT5 over SIRT1-3 and SIRT6. Biochemical studies suggest that 47 does not occupy the NAD + -binding pocket and acts as a substrate-competitive inhibitor. The identified potent and selective SIRT5 inhibitors allow further studies as research tools and therapeutic agents." @default.
- W4311779306 created "2022-12-28" @default.
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- W4311779306 date "2023-02-01" @default.
- W4311779306 modified "2023-10-14" @default.
- W4311779306 title "Pyrazolone derivatives as potent and selective small-molecule SIRT5 inhibitors" @default.
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- W4311779306 doi "https://doi.org/10.1016/j.ejmech.2022.115024" @default.
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