Fig. 4

DRV and its derivatives suppress the _M7PR but not the _M10PR or _M11PR. The chemical structures of protease inhibitors, DRV, UIC-94003, GRL-0489A, GRL-0159A , GRL-0249A and GRL-044-10A are shown in (A). All six compounds including DRV are P2 ligands [17]. Effects of the newly synthesized protease inhibitors on _mdrPR-induced growth arrest were measured against the _wtPR and _mdrPRs by using a liquid growth assay and measured by OD₆₅₀ at 48 h (B). The final drug concentration of 200 µM was used in each of the experiments. DRV was used here as a positive control and no drug treatment was used as a negative control. C Effects of the newly synthesize protease inhibitors on _mdrPR-mediated protein cleavages were tested by using the GFP-p6-Vpr fusion protein construct as described in Fig. 1A. Only the effects of UIC94003 and GRL-0489A on the _wtPR and the _M7PR were tested here because of the initial results shown in (B). DRV was used here as a positive control and no drug treatment was used as a negative control, respectively. The _mdrPR enzymatic activities were visualized under fluorescent microscopy 20 h after the gene inductions. THF, tetrahydrofuran; Cpt, cyclopentyl