IndraLab

Statements


USP14 binds IU1. 5 / 5
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reach
"IU1 and its analogs can bound to USP14 and prevent the C-terminus of ubiquitin from approaching the catalytic center55."

sparser
"The co-crystal structures indicated some important key interactions between IU1 and USP14, including a unique and delicate π-π stacking interaction, which were validated by protein point mutations and inhibitor SAR analysis."

reach
"The mechanism of action of IU1 is different from bortezomib, which inhibits the activity of the entire proteasome, whereas IU1 binds specifically and inhibits USP14 (Lim et al., 2016)."

reach
"Herein, we report the high-resolution co-crystal structures of the catalytic domain of USP14 bound to IU1 and three IU1 derivatives."

reach
"Subsequently, we performed the design and optimization of new IU1-series inhibitors, including IU1-206, based on the structural information of the interaction between IU1 and USP14 (Figure 4A)."