IndraLab

Statements

WP1130 inhibits USP5. 23 / 23
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"However, we found that several reported DUB inhibitors, including WP1130 (a known inhibitor of USP5, USP9X, USP14, USP24, and UCH37, Figure 4B), inhibit USP18 protease activity in an ISG15-Rho assay (Figure S8)."
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"WP1130 could inhibit the DUB activity of USP9X, USP5, USP14, USP37 and USP24 [ 84 ]."
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"Additionally, targeting USP5 with either WP1130 or Vialinin A suppresses USP5-mediated effects."
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"WP1130, on the other hand, inhibits at least five DUBs : USP5, UCH-L1, USP9X, USP14, and UCH37, and induces the cellular accumulation of polyubiquitinated proteins [XREF_BIBR]."
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"WP1130, an inhibitor of DUBs, can suppress the activities of USP9X, USP5, USP14 and UCH37, deregulate anti-apoptotic protein MCL-1 and upregulate pro apoptotic protein p53."
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"WP1130 inhibits USP9X, USP5, USP14, UCH37, UCH-L1 in lymphoma cells, and potentially other DUBs as well XREF_BIBR."
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"While, WP1130 mainly inhibits USP9X, USP5, USP14, and UCHL37 [23]."
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"These findings indicate that PR-619 inhibits DUB action independently of MSK1, but WP1130 inhibits DUB action, which is essential for MSK1 to increase Snail protein expression.While PR-619 is a general DUB inhibitor that inhibits many DUBs, WP1130 inhibits a subgroup of DUBs, including UCHL1, UCHL5, USP5, USP9X and USP14 (ref."
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"For example, a general DUB inhibitor WP1130 has been known to inhibit the activities of USP9x, USP5, USP14 and UCH37 that regulate the survival proteins stability [XREF_BIBR]."
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"In contrast, WP1130 is a specific inhibitor of USP5, 9X, 14, 37, and UCHL5."
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"For instance, WP1130 is designed as a relatively broad range inhibitor to block the activity of USP5, USP9X, USP14, and UCH37."
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"The same group showed, using an activity probe cell-based assay, that WP1130 inhibits USP5, USP9x and the 19S regulatory particle-associated cysteine DUBs USP14 and UCHL5 (UCH37) with an IC50 of between 5 and 10 μM [103], [104]."
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"Moreover, WP1130, which is found to be a partially selective DUB inhibitor, directly inhibits DUB activity of USP9x, USP5 and USP14 XREF_BIBR - XREF_BIBR."
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"It should be also noted, however, that G9, as well as WP1130, was recently reported to inhibit USP24 as well as USP5 in addition to USP9X [37]."
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"Kapuria et al. showed that WP1130 inhibited USP5 activity by inducing the upregulation of the proapoptotic protein p53 [92]."
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"WP1130 also reduced tumorigenicity and metastasis in a xenograft mouse model by inhibiting USP5 activity and degrading the WT1 protein [93]."
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"Assessment of DUB activity using recombinant proteins and in cell-based assays revealed that WP1130 inhibits USP5, USP9X, USP14, and UCH37, but not UCHL3."
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"WP1130 acts as a partly selective DUB inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function."
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"In Z138 mantle cell lymphoma cells, WP1130 inhibits USP9x, USP5, USP14, UCH37, UCH-L1, and potentially other DUBs XREF_BIBR."
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"WP1130 acts as a partly selective deubiquitinase inhibitor, directly inhibiting deubiquitinase activity of USP9X, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function."
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"Known as a partially selective DUB inhibitor, WP1130 inhibit USP5 activity by inducing upregulation of the pro-apoptotic protein p53 [ 83 ], whereas suppression of USP9x mediated by WP1130 leads to do[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"WP1130, a partially selective deubiquitinases (DUB) inhibitor, inhibits the deubiquitinating activities of USP5, USP9X, USP14, USP37, and UCHL1."
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"Although WP1130 is thought to inhibit other DUBs (USP5, USP14, UCH37 and UCH-L1) , the orthologous Drosophila genes were either not identified as hits in our in vivo RNAi screen or had the opposite effect to Faf, suggesting that Faf is the relevant target for WP1130 in the context of Ft regulation.However, whilst the DUB activity of Faf seems to be required for the regulation of Ft protein levels and function, it is still unclear whether Faf directly deubiquitylates Ft or if its effect is indirect."
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