IndraLab

Statements


Capzimin binds PSMD14. 5 / 5
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"Binding of capzimin and CSN5i-3 to monomeric Rpn11 and Rpn8-Rpn11 heterodimer."

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"We found that capzimin binds to RPN11 via chelation of the active site Zn and its interaction extends to the distal ubiquitin binding site."

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"Structural analysis also revealed that in the capzimin-Rpn11 complex, the Ins-1 loop and α2 helix exhibited large movements."

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"Therefore, binding of capzimin and CSN5i-3 to the monomeric Rpn11 are physiologically possible."

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"They subsequently improved the potency of 8TQ by an approach based on structure–activity relationship and identified that capzimin, a molecule that binds the catalytic site of POH1 (Fig. 3), has greatly enhanced selectivity for POH1 over other JAMM metalloenzymes and sevenfold more potency towards POH1 (IC  = 0.34 mM) [6]."