Discovery of tumor-specific irreversible inhibitors of stearoyl CoA desaturase
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چکیده
منابع مشابه
Discovery of Tumor-Specific Irreversible Inhibitors of Stearoyl CoA Desaturase
A hallmark of targeted cancer therapies is selective toxicity among cancer cell lines. We evaluated results from a viability screen of over 200,000 small molecules to identify two chemical series, oxalamides and benzothiazoles, that were selectively toxic at low nanomolar concentrations to the same 4 of 12 human lung cancer cell lines. Sensitive cell lines expressed cytochrome P450 (CYP) 4F11, ...
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A key and highly regulated enzyme that is required for the biosynthesis of monounsaturated fatty acids is stearoyl-CoA desaturase (SCD), which catalyzes the D(9)-cis desaturation of a range of fatty acyl-CoA substrates. The preferred substrates are palmitoyl- and stearoyl-CoA, which are converted into palmitoleoyl- and oleoyl-CoA respectively. Oleate is the most abundant monounsaturated fatty a...
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ژورنال
عنوان ژورنال: Nature Chemical Biology
سال: 2016
ISSN: 1552-4450,1552-4469
DOI: 10.1038/nchembio.2016