Fig. 6: Intracellular MIC assay in THP-1 macrophages.
From: Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria

a, b Exit vector 6-based Homo-BacPROTACs 7 and 8 (UdSBI-0545), as well as exit vector 7-based Homo-BacPROTACs 11 and 12 (UdSBI-4377) were assessed in a 4- and 7-day incubation on THP-1 macrophages following infection with Mtb H37Rv. The Homo-BacPROTACs were compared to their corresponding monomers (5 for exit vector 6 and 10 for exit vector 7) and the reference antibiotics rifampicin and moxifloxacin, which are known to inhibit the intracellular propagation of Mtb H37Rv. Exit vector 6 Homo-BacPROTACs showed a more efficient concentration-dependent reduction of cfu/ml over time with an Emax of 1.22 − 1.27 at 50 µM, as compared to exit vector 7 based Homo-BacPROTACs or matched monomers. The various compound concentrations are indicated in different colours, matching across the panels. CC means Mtb culture control, where no drug treatment was given. For further details see text. Error bars indicate mean ± SD of n = 2 well replicates. The CC, rifampicin and moxifloxacin values were taken as common reference points in the various graphs. Source data are provided as a Source Data file.