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phosphosite cbn pc11 biopax bel_lc signor biogrid tas lincs_drug hprd trrust | geneways tees isi trips rlimsp medscan sparser reach
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Vorinostat inhibits TP53. 9 / 17
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"LBH589 (100 nM) and SAHA (5 muM) depleted MDM2 and p53, and induced PTEN and acetyl H3 in all LPS lines."
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"XREF_BIBR, XREF_BIBR Similarly, SAHA, a histone deacetylase inhibitor, stimulates degradation of mutp53 by inhibiting HDAC6, a key positive regulator of HSP90."
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"15 described that HDAC inhibitor suberoylanilide hydroxamic acid, which shows limited clinical activity to solid tumors, reduces p53 activity in response to DNA damage."
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"SAHA downregulates mutp53 but not wtp53."
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"In the human cancer lines MDA-MB-231 (mutp53-R280K) and DLD1 (mutp53-S241F), SAHA induced a significant mutp53 degradation."
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"Additionally, vorinostat pre-treatment attenuated the stabilization of total p53 protein induced by epirubicin exposure."
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"Vorinostat pre-treatment significantly attenuated p53 stabilization in the presence of epirubicin (XREF_FIG)."
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"Vorinostat restores miR-150 and inhibits migration independently of p53 status."
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"Interestingly, the silencing of HDAC10 (XREF_SUPPLEMENTARY) resulted in the most efficient reduction of p53 (XREF_FIG), exhibiting a 25% decrease in protein expression, suggesting that the observed SAHA mediated reduction of HIF-1alpha and p53 is occurring through inhibition of different HDAC family members."
Vorinostat inhibits mutated TP53. 9 / 9
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"Specifically, suberoylanilide hydroxamic acid (SAHA, also known as vorinostat), a FDA approved HDACi that inhibits class I, II, and IV HDACs, induces degradation of mutant p53 by inhibiting HDAC6 activity, an essential positive regulator of Hsp90, and subsequent disruption of the HDAC6/Hsp90/mutant p53 complex, leading to mutant p53 ubiquitination by MDM2 and CHIP."
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"To further explore whether inhibitors of HSP90 and HDACs are capable of inducing Pirh2 expression to degrade mutant p53, HaCaT and MIA PaCa-2 cells were treated with 17AAG or SAHA."
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"Vorinostat did not completely inhibit the mutant p53 population, and this was reflected in the estimated inhibitory coefficient for mutant p53 (I mp53 = 0.202 muM -1; Table 1)."
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"cl.PARP.BCL-xL; BcL-xL (0) = 1 Vorinostat stimulates wild type p53 (wtp53) and inhibits mutant p53 (mp53) expression.10, 19, 20 In this study, p53 initially decreased, began to return to baseline around 24 hours, and eventually increased beyond the baseline."
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"Importantly, we could demonstrate for the first time that the HDAC inhibitor SAHA is able to effectively and specifically downregulate mutant p53 protein by promoting its degradation, while having no effect on wild-type p53 protein levels (XREF_FIG)."
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"Vorinostat sensitized DU145 cells to PARPi/IR and decreased mutant p53."
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"It is known that SAHA induces the degradation of mutant p53 protein via inhibiting HDAC6, a member of class IIb HDACs."
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"We found that mutant p53 protein was markedly decreased by ATO, 17AAG, or SAHA, and further decreased by combination of ATO with 17AAG or SAHA (XREF_FIG)."
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"Wang et al. described that SAHA causes a massive reduction of mutant p53 through the disruption of the physical interaction between YY1 and HDAC8 [XREF_BIBR]."
Vorinostat inhibits TP53-R270H. 2 / 2
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"For the inhibition of p53 R270H, organoids were treated with pan-histone deacetylase inhibitor suberoylanilide hydroxamic acid (Sigma)."
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"28 We confirmed that SAHA treatment abolished the nuclear accumulation of p53 R270H in Apc Delta716 Trp53 R270H and R270H organoids in a dose dependent manner (XREF_FIG)."