IndraLab

Statements

P5091 inhibits MDM2. 10 / 10
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"Co-immunoprecipitation assays show that HDM2 is associated with p21 in MM cells, and that P5091 downregualates HDM2 and upregualtes p21 (XREF_FIG)."
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"P5091 downregulated MDM2 and upregulated p53 in WI‐38 SnCs but not in WI‐38 non‐SnCs (Figure 1c)."
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"Notable examples include FOXO-DRI, which activates FOXO transcription factors involved in regulating the cell cycle and apoptosis [219]; UBX0101, known for its ability to selectively induce apoptosis in senescent cells, offering therapeutic promise for age-related diseasesm [219]; and P22077/P5091, which inhibit MDM2 to enhance P53 activity and promote the removal of senescent cells [220]."
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"Examination of harvested tumors showed that P5091 inhibited USP7 activity, decreased HDM2, and increased p21 levels relative to tumors from control mice (XREF_FIG)."
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"P5091 accelerates the degradation of HDM2 versus control cycloheximide (CHX) alone treated U20S cells (XREF_FIG)."
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"Likewise, P5091 enhanced the degradation of HDM2 in prostate cancer cell lines (XREF_SUPPLEMENTARY)."
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"The functional specificity of P5091 is confirmed using different strategies : first, cell-free based experiments using a reporter (Ub-PLA 2)-based assay demonstrate a potent, specific, and selective inhibition of USP7 activity by P5091; second, P5091 enhances degradation of its primary substrate HDM2; third, USP7 KO in HCT-116 cells confers resistance to P5091; and fourth, P5091 blocks USP7 DUB activity without altering proteasome activity."
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"Western blot analysis revealed that P5091 decreased the level of MDM2 protein that is otherwise induced by ATSP-7041 as a result of the surge in p53 and counter-up-regulation of MDM2 (XREF_FIG)."
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"22 Combination of RRx-001 and P5091 markedly decreased HDM2, upregulated p53 and p21 versus either agent alone (XREF_FIG)."
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"For example, in the case of ATSP-7041 and P5091 treatment, the addition of P5091 suppresses the counter up-regulation of MDM2."
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