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Aug 2026

Substrate Mimicry by Inhibitors of the Mycobacterium tuberculosis 20S Proteasome and Their Activity against Mycobacteria In Vitro and in Macrophages

The remarkable and problematic capacity of Mycobacterium tuberculosis to persist in the host is dependent on a functional 20S proteasome that is structurally and functionally analogous to its mammalian counterpart. It has been proposed that this enzyme is critical for the bacterium’s adaptive response to a variety of...

Xilin Gu, Peter J. Rowheder, Zanlin Yu et al. · 0 citations

Structure − Activity Relationship Study of Antimalarial Asparagine-Derived Proteasome Inhibitors

Cryo-EM structural studies reveal a novel binding pose of the inhibitor at the Pf 20S β 5 active site, explaining the enhanced activity of an N -cap sulfonamide modification compared to an N -cap amide, and offer insights into the development of next-generation antimalarial Pf 20S-targeting compounds with improved drug...

Hao Zhang, Da-Qiang Li, Hao-Chi Hsu et al. · 0 citations

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