The enzyme was preincubated for 5 min at 35°C with the various reagents before addition of the substrate. Each reagent was added at the final concentration as indicated.
Values are expressed as mean values ± standard deviation (n = 3 experiments); %, percentage;*, 8 mg/ml in the reaction medium;**, 0.4 mg/ml;***, 100 µg/ml in the reaction medium;A, B, C, D: means foll
Compounds 1–7 ranked according to potency (in bold) have no activity against additional targets based on polypharmacology records, whereas compounds 8–12 inhibit calcitriol activating enzymes, VDR and
casein zymographic analysis demonstrates the significant increase in MMP-12 activity (P<0.01) in COPD mice compared to control mice. This increase was significantly inhibited in mice exposed to PM2