IndraLab

Statements

Capzimin inhibits PSMD14. 5 / 5
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"Capzimin and clioquinol are two proteasome inhibitors that function through different mechanisms: Capzimin inhibits the isopeptidase activity of the proteasomal subunit RPN11 [23], while clioquinol acts as an ionophore, directing metal ions to disrupt the proteasomal enzymatic complex [24]."
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"Capzimin (quinolone-8-thiol (8TQ)) selectively inhibits the proteasomal DUB Rpn11 and POH1 through direct binding to the catalytic Zn 2+ ion in POH1 's active site."
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"Capzimin blocks proteasome function by inhibiting the deubiquitinase activity of Rpn11, which causes accumulation of polyubiquitinated proteins, triggers the UPR, and blocks cell proliferation [40]."
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"Pharmacological inhibition of RPN11 by Capzimin ameliorated NAFLD, NASH, and related metabolic disorders in mice and reduced lipid contents in human hepatocytes cultured in 2D and 3D."
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"Capzimin is a selective inhibitor of Rpn11 while CSN5i-3 is selective for CSN5."
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