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

Hao Zhang Da-Qiang Li Hao-Chi Hsu Akshay Vishwanatha Wen-Hu Zhan Takafumi Yukawa Joseph E. Visone T. Imaeda R. Okamoto Pavla Fajtová Ryoma Hara M. Kawasaki Kenjiro Sato M. Michino Shreeya Garg O. Kreutzfeld Patrick K. Tumwebaze Stephen Orena Martin Okitwi K. Aso R. Cooper Philip J. Rosenthal Peter T. Meinke M. Foley A. J. O'Donoghue Hui-Lin Li L. Kirkman G. Lin
· 0 citations · 14 references

TL;DR

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-like properties.

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