Proteasome Inhibitors Show Promise For Drug-Resistant Malaria (IMAGE)
Caption
In silico modeling of the Plasmodium falciparum 20S proteasome bound by the covalent parasite-selective WLL peptide-based inhibitor. (A) Docking of WLL into the wild-type b5 site of the cryo-electron microscopy-derived 20S parasite proteasome model. The b5 and b6 subunits are in light blue and dark blue, respectively. (B) Molecular dynamic simulations illustrate how the b5 A20S mutation affords low-level resistance to WLL by reducing compound binding to the b5 active site. Arrow highlights the WLL P3 tryptophan residue.
Credit
Stokes, et al. (2019)
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