IndraLab

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USP9X inhibits Neoplasms. 7 / 8
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"Furthermore, the expression level of USP9X is positively related to LATS expression but negatively associated with the expression of YAP/TAZ in multiple tumor tissues, such as pancreatic cancer and breast cancer, demonstrating that USP9X potentiates LATS kinase in suppressing tumor growth (Toloczko et al., 2017)."
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"The pharmacological inhibition of USP9x using G9, a partially selective, small-molecule USP9x inhibitor, reduced Notch activity, remodeled the tumor immune landscape, and reduced tumor growth without associated toxicity."
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"For example, USP9X inhibits the formation of colon tumors by stabilizing FBW7 protein [25]."
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"Using PANC-1 PC cell line, USP9X was reported to promote tumor metastasis and inhibit tumor apoptosis [ 34 ]."
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"Consistent with the functions in vitro and in bulk cell population (Fig. 5A–C and Fig. 2E), within both in vivo imaging and anatomical assays, USP9X deprivation suppressed the tumor regeneration and intraperitoneal metastasis capability of CSCs."
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"However, USP9X may also suppress tumor development in the pancreas if certain tumor suppressive contexts are provided, i.e., activation of a scaffold protein that can link USP9X with a tumor suppressor whose deubiquitination leads to its stabilization and activation in pancreatic cells.The double-sidedness of USP9X action seems to make it difficult to develop specific, targeted clinical inhibitors despite its good druggability as an enzyme."
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"In a mouse xenograft model of triple negative breast cancer (negative for the estrogen, progesterone, and HER2 receptors), the FAF/Rapa formulation potently inhibited tumor growth and exhibited a better toxicity profile compared to free Rapa control."
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