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. 2022 Sep 22;13:5555. doi: 10.1038/s41467-022-33148-5

Fig. 2. Characterization of the mode of action of PXS-4787.

Fig. 2

a Lysyl oxidase inhibitory profile of PXS-4787 (n = 11). b Time-dependent increase in potency of PXS-4787 (n = 12 at each timepoint). c Irreversible inhibition of LOXL1, LOXL2, and LOXL3 by PXS-4787 and BAPN as measured in a jump dilution assay and compared to a reversible inhibitor. d Substrate (putrescine) competition showing a reduction of potency with increasing substrate concentration due to competition for the enzymatic pocket. e Postulated mechanism of irreversible inhibition by PXS-4787. f Oxidation of PXS-4787 and BAPN by SSAO (n = 2–4 independent experiments, p values 0.0097, 0.058 for 30 and 60 micromolar concentration, respectively). g Oxidation of PXS-4787 and BAPN by DAO (n = 2–4 independent experiments, p values < 0.0001, 0.012 and 0.019 for 30, 600 micromolar concentration respectively). Data are expressed as mean ± SEM. Subsequent statistical analysis was performed with unpaired two-sided Student’s t tests. *p < 0.05, **p < 0.01, ***p < 0.001and ****p < 0.0001. Source data are provided as a Source Data file.