IndraLab

Statements


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"Pimozide and GW7647 inhibit USP1 and UAF1 by a noncompetitive mechanism."

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"In order to demonstrate that pimozide and GW7647 inhibit the USP1 and UAF1 activity in cells, we developed an assay to determine the levels of Ub-PCNA or Ub-FANCD2 in cells treated with cisplatin, pimozide and GW7647 or a combination of cisplatin and pimozide and GW7647."

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"In this study, we showed that pimozide is a potent inhibitor of a human DUB, USP1 and UAF1, and provided insight into the molecular basis for the antineoplastic activity of pimozide."

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"It is worth noting that pimozide could down-regulate ULK1-related autophagy by inhibiting USP1."

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"For instance, the specific inhibition of USP1 by pimozide has been demonstrated to effectively suppress GSCs [183]."

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"Another study confirmed that pimozide could inhibit USP1 and in turn decrease the clonal growth of glioblastoma cells as well as increase their sensitivity to irradiation, though they are commonly resistant to chemotherapeutic and irradiation treatments."

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"Further studies of the USP1/UAF1 inhibitors suggested that pimozide and GW7647 inhibit USP1/UAF1 by a non‐competitive mechanism and bind at a site other than the active site of USP1/UAF1 [113]."

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"Pimozide seems to inhibit pEGFR and USP1, which stabilizes—via deubiquitination—the ID1 protein, and has proved its efficacy against multiple tumor pathways at in vivo mouse models too, underlying a new potential drug combination against TMZ-resistant GBs [29,30]."

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"Pimozide increases proteasomal degradation of ID-1 by blocking USP1, a ubiquitin-specific protease responsible for deubiqutination of ID-1 [255,256]."

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"Pimozide and GW7647 inactivate USP1 and UAF1 in cells."