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B-AP15 inhibits UCHL5. 22 / 22
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"In line with this, Tian et al. reported that b-AP15 selectively blocks deubiquitylating activity of USP14 and UCHL5, leading to the inhibition of cell growth and overcoming bortezomib resistance in MM cells [XREF_BIBR]."
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"It is known that b-AP15 and PtPT can inhibit the activity of both USP14 and UCHL5 simultaneously, implying that the downregulation of ERα by b-AP15 and PtPT may attribute to the suppression of USP14 and UCHL5."
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"Inhibition of USP14 and UCH37 deubiquitinating activity by b-AP15 as a potential therapy for tumors with p53 deficiency."
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"Inhibition of USP14 and UCH37 deubiquitinating activity by b-AP15 as a potential therapy for tumors with p53 deficiency."
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"These data and the fact that UCH37 or USP14 may have a redundant DUB function and also that b-AP15 and WP1130 inhibit both UCH37 and USP14 suggests that a contribution from both enzymes may be needed."
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"Although the results obtained by D’Arcy and colleagues demonstrate that b-AP15 is an inhibitor of USP14/UCH-37, two unrelated cysteine protease enzymes from different DUB families, the chemical structure of b-AP15 suggests additional proteins may be targeted by this compound and its analogues."
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"XREF_BIBR These results have also been further supported by the findings of the Feng et al XREF_BIBR study which have shown that b-AP15 inhibits the deubiquitylating activity of USP14 and UCHL5 enzymes, triggering apoptosis in MM cell lines in a time dependent and dose dependent manner."
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"Although the mechanism for the observed UPS inhibition has not been completely elucidated, we found that b-AP15 selectively inhibited the proteasome-associated deubiquitinases (DUBs) USP14 and UCHL5 at IC -IC concentrations."
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"B-AP15 (WO2013058691) is an inhibitor of USP14 and UCHL5 associated with 19S RP that has been found to inhibit the progression of tumors in certain human cancers as well as mouse cancer models of lung[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Hence, we speculated that Aur inhibited androgen receptor signaling by PKC pathway and promoted the degradation of androgen receptor result from USP14 and UCHL5 inhibition.Interestingly, inhibition of[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In contrast to inhibitors of the 20S proteasome, b-AP15 blocks the deubiquitylating activity of USP14 and UCHL5, which are associated with the 19S regulatory particle, without affecting proteolytic activities of the 20S proteasome [XREF_BIBR, XREF_BIBR, XREF_BIBR]."
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"Further studies indicated that b-AP15 is an inhibitor of both USP14 and UCHL5 and has an IC50 value of 2.1 muM when using purified 19S proteasome [XREF_BIBR]."
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"Thus, b-AP15 can inhibit the Ub chain trimming enzymes Uch37 and Usp14 of the 26S proteasome, functions similarly to proteasome inhibitors when used to treat cells, and has potential uses in cancer therapy."
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"VLX1570 and b-AP15 both inhibit USP14 and UCHL5 activity of 19S regulatory particles with the inhibition of USP14 being more pronounced (XREF_FIG)."
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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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"There are some debates over whether b-AP15 can block not only UCH-L5 and USP14 but also inhibit POH1 ."
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"B-AP15 inhibits both UCH37 and USP14 , and induces accumulation of ubiquitinated substrates [ 214 ] ."
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"SERPB12 has been predicted to bind to USP14 in hepatocellular carcinoma tissues [XREF_BIBR], so we tested whether b-AP15, which inhibits the deubuiquitylases (DUB) UCHL5 and USP14 [XREF_BIBR] could block SLFN12 effects."
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"A similar phenomenon is seen with b-AP15 and VLX1570 that are reported to inhibit the proteasomal DUBs UCH37 and USP14."
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"Finally, b-AP15 specifically inhibits two proteasome associated DUBs : UCH-L5 and USP14, and thus blocks proteasome function leading to the accumulation of polyubiquitin in treated cells [XREF_BIBR]."
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"Of the commonly used DUB inhibitors, b-AP15 blocks the DUB activity of both Uchl5 and Usp14 (D'Arcy et al., 2011) and IU1 inhibits specifically Usp14 activity (Lee et al., 2010)."
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"Although IU1 and IU1-47 are reported to be specific for USP14 (Boselli et al., 2017; Lee et al., 2010), b-AP15 is believed to inhibit the proteasomal deubiquitinating activity of both USP14 and UCH37 (D'Arcy et al., 2011)."
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