IndraLab

Statements

IU1 inhibits USP14. 28 / 28
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"IU1 is a specific inhibitor of USP14 vs. other human DUBs including 19S proteasome DUBs, which is also able to enhance the proteasome activity [XREF_BIBR]."
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"The small-molecule IU1 inhibits specifically USP14 with an IC 50 of 4-5 microM [XREF_BIBR]."
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"Superimposition of USP14 -IU1 with USP14-Ubal demonstrated that IU1 inhibits USP14 by blocking the entrance of the ubiquitin C-terminus into the thumb-palm cleft where the catalytic center is buried (Figure 4A) (Wang et al., 2018)."
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"IU1 inhibits USP14 by preventing its docking on the proteasome and increases K63-ubiqutination of Beclin1 ( ref ."
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"USP14 inhibition by either IU1 or specific shRNA dramatically decreased the colony formation of MDA-MB-453 and MDA-MB-231 cells after 2 weeks; however, the identical experimental conditions had little or no inhibitory effect on T47D colonies."
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"Similar to the effect of Usp14 knockout, wild-type MEFs treated with IU1 showed significantly reduced LRP6 phosphorylation (XREF_FIG)."
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"IU1 is an inhibitor of the proteasome associated DUB Usp14."
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"A compound (IU1) has been identified to specifically inhibit USP14."
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"Lee and his colleagues showed that IU1 specifically inhibits USP14 activity of the proteasome and thereby enhances proteasomal degradation of the substrates [78]."
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"The small molecule inhibitor of USP14, IU1, was identified by high-throughput screening, and found to enhance proteasomal degradation of target substrates in vitro and in vivo7."
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"Therefore, suppression of USP14 by IU1 improves animal survival and enhances functional recovery."
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"Collectively, these data demonstrated that USP14 promoted HCC proliferation and tumor growth.To further verify whether ablation of USP14 or/and a selective deubiquitination activity inhibitor of USP14 (IU1) could restrain HCC growth in animals, we implanted subcutaneously USP14-depleted HCCLM3 cells stably expressing USP14-specific shRNA (shUSP14) or control shRNA (shCtrl) and monitored tumor growth as they were treated with IU1 or vehicle (Figure S4A, B)."
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"A small molecule inhibitor of the DUB USP14 was identified through a high through put screen called IU1 (inhibitor of USP14) [254]."
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"Both studies have clearly shown that IU1 inhibits Usp14, b-AP15 inhibits Usp14 and Uch37, and neither inhibitor abolishes the activity of several other tested DUBs."
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"Importantly, a synergic effect of oral administration of IU1 in combination with lentivirus-mediated USP14 knockdown on tumor growth inhibition was observed upon co-treatment of the two different ways to inhibit USP14 for 14 days (Fig. 8A)."
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"Although overexpression of USP14 is not sufficient to polarize macrophages to the M2 phenotype, inhibition of USP14 by IU1 in tumor-bearing mice disrupts the suppressive activity of cancer-promoting macrophages and effectively reshapes immune microenvironment characteristics."
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"Firstly, to determine the underlying effect of IU1 (a selective inhibitor of USP14) on the proliferation of cervical cancer cells, we used the CCK-8 assay."
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"Inhibition of Usp14 by IU1 is reversible and likely acts on the catalytic site of Usp14 [XREF_BIBR]."
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"[ 62,63 ] IU1 was shown to inhibit Usp14 , resulting in proteasome activity promotion ."
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"Inhibition of USP14 by IU1 caused a concentration dependent, significant suppression on the proliferation of MDA-MB-453, MDA-MB-231, and MCF7 carcinoma cells."
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"As I/R is associated with oxidative stress, protein and organelle damages, as well as accumulation of ubiquitinated protein aggregates, we next examined whether inhibition of USP14 by IU1 alters the accumulation of protein aggregates."
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"In addition, IU1 enhances proteasomal degradation by inhibiting USP14, a proteasome associated DUB."
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"IU1 inhibits USP14 in the proteasome specifically and reversibly with a low-micromolar IC 50 in vitro and accelerated substrate degradation by proteasome in cells."
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"On the other hand, it is also possible that the IU1 induced neuroprotection in the post-ischemic mouse brains is a synergistic effect of multiple pathways activated by suppression of USP14 through IU1, since recent results suggest that inhibition of USP14 by IU1 in vitro elevates autophagy activity."
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"Inhibition of USP14 by IU1 may cause unexpected cellular responses."
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"IU1 could potentially inhibit Usp14 by preventing its docking on the proteasome, but direct tests of this scenario proved negative (XREF_SUPPLEMENTARY)."
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"In conclusion, we report that IU1 inhibits USP14 by binding to the thumb-palm cleft region of the USP14 catalytic domain, which prevents the substrate from binding to the enzyme."
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"The mechanism of action of IU1 is different from bortezomib , which inhibits the activity of the entire proteasome , whereas IU1 binds specifically and inhibits USP14 ( Lim et al ., 2016 ) ."
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