Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome.
Xie, S.C., Metcalfe, R.D., Mizutani, H., Puhalovich, T., Hanssen, E., Morton, C.J., Du, Y., Dogovski, C., Huang, S.C., Ciavarri, J., Hales, P., Griffin, R.J., Cohen, L.H., Chuang, B.C., Wittlin, S., Deni, I., Yeo, T., Ward, K.E., Barry, D.C., Liu, B., Gillett, D.L., Crespo-Fernandez, B.F., Ottilie, S., Mittal, N., Churchyard, A., Ferguson, D., Aguiar, A.C.C., Guido, R.V.C., Baum, J., Hanson, K.K., Winzeler, E.A., Gamo, F.J., Fidock, D.A., Baud, D., Parker, M.W., Brand, S., Dick, L.R., Griffin, M.D.W., Gould, A.E., Tilley, L.(2021) Proc Natl Acad Sci U S A 118
- PubMed: 34548400 
- DOI: 10.1073/pnas.2107213118
- Primary Citation of Related Structures:  
7LXT, 7LXU, 7LXV - PubMed Abstract: 
The Plasmodium falciparum proteasome is a potential antimalarial drug target. We have identified a series of amino-amide boronates that are potent and specific inhibitors of the P. falciparum 20S proteasome ( Pf 20S) β5 active site and that exhibit fast-acting antimalarial activity ...