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- W2026497502 abstract "Membrane-associated serine protease matriptase has been implicated in human diseases and might be a drug target. In the present study, a novel class of matriptase inhibitors targeting zymogen activation is developed by a combination of the screening of compound library using a cell-based matriptase activation assay and a computer-aided search of commercially available analogues of a selected compound. Four structurally related compounds are identified that can inhibit matriptase activation with IC50 at low micromolar concentration in both intact-cell and cell-free systems, suggesting that these inhibitors target the matriptase autoactivation machinery rather than the intracellular signaling pathways. These activation inhibitors can also inhibit prostasin activation, a downstream event that occurs in lockstep with matriptase activation. In contrast, the matriptase catalytic inhibitor CVS-3983 at a concentration 300-fold higher than its Ki fails to inhibit activation of either protease. Our results suggest that inhibiting matriptase activation is an efficient way to control matriptase function." @default.
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- W2026497502 date "2011-10-12" @default.
- W2026497502 modified "2023-10-04" @default.
- W2026497502 title "Targeting Zymogen Activation To Control the Matriptase-Prostasin Proteolytic Cascade" @default.
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- W2026497502 doi "https://doi.org/10.1021/jm200920s" @default.
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