| Assay Method Information | |
| | Inhibition of the S. maltophilia L1 MBL |
| Description: | On the basis of these in vitro data we conclude that the bicyclic boronate 2 acts against S. maltophilia in a similar fashion to avibactam and clavulanic acid in its ability to reverse aztreonam and (when due to L1/L2 hyperproduction) ceftazidime resistance (Table 2). As to date the inhibition of class B3 MBLs by bicyclic boronates has not been reported, we investigated the inhibition of purified L1 and L2 by the three inhibitors using the fluorogenic β-lactamase substrate FC5 as a reporter. Steady-state kcat/KM values clearly demonstrate that FC5 is hydrolysed with high efficiency by both L1 and L2 (Table 1). IC50 measurements revealed that while all three compounds inhibit L2 with nanomolar potencies (Table 5), no inhibition of L1 was observed for any of the three inhibitors, even when using inhibitor concentrations up to 2.5 mM. |
| Affinity data for this assay | |
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