IndraLab

Statements


Pimozide activates USP1. 4 / 4
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"The top inhibitors, pimozide and GW7647, inhibited USP1 and UAF1 noncompetitively with a K i of 0.5 and 0.7 muM respectively, and displayed selectivity against a number of deubiquitinases, deSUMOylase and cysteine proteases."

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"The most potent inhibitors, pimozide and GW7647, inhibited USP1 and UAF1 reversibly with a micromolar IC 50."

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"The top inhibitors, pimozide and GW7647, blocked USP1 and UAF1 noncompetitively with a Ki of 0.5 and 0.7 muM, respectively, and displayed selectivity against a number of deubiquitinases, deSUMOylase, [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"In addition, pimozide inhibits the proliferation of human melanoma and breast cancer cells (Neifeld et al. 1983; Strobl 1990) and is able to reverse the chemo resistance of non-small cell lung cancer cells to the DNA cross-linker, cisplatin, further supporting USP1/UAF1 as a potential target for novel anticancer therapy (Chen et al. 2011) (Table 11.3)."
| PMC