IndraLab

Statements


P5091 increases the amount of CDKN1A. 5 / 5
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"P5091 (XREF_TABLE) actively inhibits USP7 at concentrations as low as 5-10 microM in the cellular environment, resulting in HDM2 polyubiquitination and accelerated degradation by the proteasome, and consequently increased steady-state protein levels of p53 and p21."

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"Second, P5091 treatment decreases the viability of p53-null ARP-1 MM cells (XREF_FIG), associated with decreased HDM2 levels and increased p21 expression (XREF_FIG, inset)."

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"Mechanistic studies further show that P5091 triggered apoptosis in MM cells is associated with 1) activation of caspase-8, caspase-9, caspase-3, and PARP; and 2) downregulation of USP7 substrate HDM2, as well as increased expression of p53 and p21."

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"P5091 increased p53 and p21 protein levels in a time dependent fashion in the wild-type TP53 cells, TC32 and TC138 (XREF_FIG)."

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"Notably, P5091 treatment decreased the viability of p53 null ARP-1 MM cells, associated with decreased Mdm2 levels and increased p21 expression."