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P5091 inhibits USP7. 38 / 38
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"P5091 (inhibitor of USP7) and b-AP15 (inhibitor of USP14/UCHL5) inhibit the growth of bortezomib-resistant multiple myeloma [41,42,]."
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"The binding of P5091 in this state possibly block USP7 into auto-inhibited state by reducing the elasticity of the pocket residues drastically."
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"P5091 can effectively block the deubiquitinating activity of USP7, leading to the destabilization of its oncogenic substrates such as FOXM1, oncoprotein SE translocation (SET), and N-myc [27, 52, 53]."
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"Chauhan et al 14 discovered that P5091 was a specific inhibitor of deubiquitylating enzyme USP7."
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"Moreover, the inhibition of USP7 by P5091 accelerated the degradation of CCDC6 versus control in cycloheximide treated SCLC cells in vitro and sensitized the cells to PARP inhibitors alone and in combination with cisplatin (71)."
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"After USP7 inhibition by P5091, the PE decreased significantly in both cell lines analyzed."
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"P5091 is an inhibitor of USP7 and USP47 ( Chauhan et al., 2012; Weinstock et al., 2012 ) and was found to induce apoptosis of multiple myeloma cells resistant to the 20S proteasome inhibitor bortezomi[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"As expected, mice in which USP7 activity was inhibited by P5091 showed dramatically increased susceptibility to Salmonella typhimurium."
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"P5091 , as an inhibitor of USP7 , actively inhibits USP7 , resulting in increased steady-state protein levels of p53 and p21 ."
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"The study has also suggested that P5091 inhibits USP7 activity without blocking proteasome function directly."
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"P5091 has been shown to inhibit tumor growth by inhibiting USP7 and USP47 and is well tolerated in animals [107] ."
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"USP7 inhibition by P5091 can drive macrophage reprogramming, while reduced Treg suppressive function was not observed under USP7 blockade [52, 91]."
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"By Western blot analysis, we showed that MDM2 was slightly decreased in both parental and USP22-Ko A549 cancer cells, while USP22 was significantly upregulated by P5091 treatment (Fig. 6D), which confirms that P5091 effectively inhibited USP7 deubiquitinase activity."
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"P5091, as an inhibitor of USP7, actively inhibits USP7, resulting in increased steady-state protein levels of p53 and p21."
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"Also P5091 and P22077 can inhibit USP7 with moderate activity and selectivity, related research on the structural basis for binding to USP7 has not been reported so far.We carried out molecular dockin[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"However, the commercially available inhibitors for these DUBs had no obvious influence on the SOX2 expression, including b-AP15 (the inhibitor of USP14 and UCHL5), P5091 (the inhibitor of USP7 and USP[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Here we show that P5091 is an inhibitor of deubiquitylating enzyme USP7, which induces apoptosis in MM cells resistant to conventional and bortezomib therapies."
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"P5091 is a selective inhibitor of USP7."
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"P5091 inhibited the labeling of USP7 with HA-UbVME in a concentration dependent manner (XREF_FIG)."
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"Inhibition of USP7 by P5091 (compound 1) was shown to cause apoptosis of multiple myeloma cells and prolonged survival in animal xenograft models ( Chauhan et al., 2012 )."
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"P5091 inhibits USP7 deubiquitylating activity, without blocking proteasome activity, in MM cells."
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"P5091 cause significant inhibition (> 50%) of USP7 activity in a concentration dependent manner (XREF_FIG)."
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"The selective inhibitor of USP7, P5091, has also been found to promote bone repair and homeostasis in osteoporotic conditions."
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"These data suggest that P5091 blocks USP7 activity without altering proteasome function."
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"P5091 blocks the USP7 activity in MM at the IC 50 of P5091 for these cells (XREF_FIG and data not shown)."
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"It has been reported that USP7 inhibition by P5091 for CRC inhibition is p53-independent.32 Both p53 and PTEN show no mutation in CT26.33 Also, the antitumor immunity in the microenvironment was specifically examined."
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"Initial biochemical characterization revealed that P5091 selectively inhibited USP7 relative to other DUBs and other families of proteases, and subsequent medicinal chemistry optimization generated ad[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Finally, it is noteworthy that P5091-mediated USP7 inhibition resulted in increased PD-L1 expression in tumor cells."
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"Ubiquitin ligase inhibitors under development include P5091 targeting USP-7 which can overcome Bortezomib resistance in vitro [5] and b-API15 targeting USP14 which is entering clinical trials [6]."
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"Together, these results show that USP7 inhibition by P5091 and P217564 selectively interferes with the immunosuppressive functions of regulatory T cells, while preserving other important host T cell antitumor responses."
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"In vivo, blockade of USP7 by P5091 facilitated the recruitment of IFN-γ CD8 T cells, accompanied by PD-L1 downregulation, which synergized with ICB to retard Lewis lung cancer growth [52] (Table 1)."
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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 is an active inhibitor of USP7, and the CCK8 assay results suggested that 5 ​μM P5091 had no significant effect on cell activity (Supplementary Figure S3A)."
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"When further analyzed by Western blot, we found that the inhibition of USP7 by P5091 in AZD/NaCr-treated cells partially reduced TRIM27 protein."
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"Using the combination of P5091 (an inhibitor of USP7) and PD-1 monoclonal antibody, researchers were able to demonstrate a synergistic anti-tumor impact, which bodes well for the future of lung cancer therapy.96 Furthermore, in gastric cancer, the amount of PD-L1 is favorably linked with the level of USP7."
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"Importantly, P5091 inhibits USP7 activity in vivo and induces apoptosis in MM xenografted tumors."
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"Moreover, some USP7 selective inhibitors, including HBX41,108, HBX19,818, HBX28,258, P022077, P5091, and P22077, have been characterized using fluorescence based high-throughput screening [XREF_BIBR - XREF_BIBR]."
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"We observed that the level of CRIP1 was obviously downregulated if the USP7 activity was repressed by the treatment with P5091 (a USP7 inhibitor) in both wild-type and CRIP1-OE MM cells in a dose-dependent manner."
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