Fig. 5: Pharmacokinetic-pharmacodynamic measurement of target engagement in rat skin in vivo. | Nature Communications

Fig. 5: Pharmacokinetic-pharmacodynamic measurement of target engagement in rat skin in vivo.

From: Topical application of an irreversible small molecule inhibitor of lysyl oxidases ameliorates skin scarring and fibrosis

Fig. 5

Dose-dependent reduction of lysyl oxidase activity in rat skin following a  single dose (a) (p = 0.0269) or (b) repeated application of cream (p = 0.0007, p = 0.0002, p < 0.0001 for 0% vs 0.5%, 1% and 3% respectively). Activity was measured 24 h after last topical application. Noise in these assays was determined by measuring background fluorescent changes in the presence of a high (>300 μM) concentration of BAPN to block all lysyl oxidase activity in the presence of other amine oxidase inhibitors (n = 3 per group). The signal (activity in the absence of BAPN) over noise (signal of the same extract in the presence of BAPN). Statistical analysis was performed with one-way ANOVA with Tukey’s method for multiple comparisons. *p < 0.05, **p < 0.01, ***p < 0.001 and ****p < 0.0001. Source data are provided as a Source Data file.

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