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TG2-179-1 inhibits BAP1. 7 / 7
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"TG2-179-1 inhibits the DUB activity of BAP1 by binding to its active site."
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"We then determined whether TG2-179-1 inhibits BAP1 using purified recombinant BAP1 proteins and the fluorogenic artificial DUB substrate Ub-AMC as a BAP1 substrate."
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"In support of this prediction, TG2-179-1 inhibited BAP1 even after immunoprecipitation of TG2-179-1-bound BAP1 with extensive washing."
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"Incubation of BAP1 with increasing concentrations of TG2-179-1 reduced the emission of fluorescence from Ub-AMC in a dose-dependent manner (Fig. 5C), indicating that TG2-179-1 inhibited the DUB activity of BAP1."
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"TG2-179-1 inhibited the DUB activity of BAP1 toward nucleosomal H2A-Ub substrates in a dose-dependent manner (Fig. 5D)."
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"Having verified that TG2-179-1 inhibits BAP1, we investigated its impact on the viability of colon cancer cells."
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"However, TG2-179-1 kills both BAP1-insensitive and BAP1-depleted colon cancer cells as well as BAP1-null mesothelioma and ccRCC cells, indicating that TG2-179-1 targets BAP1 as well as other cellular proteins."
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