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- W2091992166 abstract "Inhibition of caspase-6 is a potential therapeutic strategy for some neurodegenerative diseases, but it has been difficult to develop selective inhibitors against caspases. We report the discovery and characterization of a potent inhibitor of caspase-6 that acts by an uncompetitive binding mode that is an unprecedented mechanism of inhibition against this target class. Biochemical assays demonstrate that, while exquisitely selective for caspase-6 over caspase-3 and -7, the compound’s inhibitory activity is also dependent on the amino acid sequence and P1’ character of the peptide substrate. The crystal structure of the ternary complex of caspase-6, substrate-mimetic and an 11 nM inhibitor reveals the molecular basis of inhibition. The general strategy to develop uncompetitive inhibitors together with the unique mechanism described herein provides a rationale for engineering caspase selectivity." @default.
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- W2091992166 date "2012-12-05" @default.
- W2091992166 modified "2023-10-12" @default.
- W2091992166 title "Mechanistic and Structural Understanding of Uncompetitive Inhibitors of Caspase-6" @default.
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- W2091992166 doi "https://doi.org/10.1371/journal.pone.0050864" @default.
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