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• W2299722030 abstract "An active site mapping of human cathepsin B with dipeptide nitrile inhibitors was performed for a combinatorial approach by introducing several points of diversity and stepwise optimizing the inhibitor structure. To address the occluding loop of cathepsin B by a carboxylate moiety, click chemistry to generate linker-connected molecules was applied. Inhibitor 17 exhibited K i values of 41.3 nM, 27.3 nM, or 19.2 nM, depending on the substrate and pH of the assay. Kinetic data were discussed with respect to the conformational selection and induced fit models." @default.
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• W2299722030 date "2016-01-12" @default.
• W2299722030 modified "2023-09-24" @default.
• W2299722030 title "Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry" @default.
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• W2299722030 doi "https://doi.org/10.1021/acsmedchemlett.5b00474" @default.
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