Abstract
A key step in the onset of Huntington's disease is the caspase-6 mediated cleavage of the protein huntingtin into toxic fragments. Therefore, the inhibition of caspase-6 has been identified as a target for therapeutic drug development for the treatment of this disease. In this study, a series of isatin sulfonamide Michael acceptors having a high nanomolar potency for inhibiting caspase-6 and increased selectivity for caspase-6 versus caspase-3 inhibition is reported.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Caspase 3 / chemistry
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Caspase 6 / chemistry
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Caspase Inhibitors*
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Humans
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Isatin / analogs & derivatives*
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Isatin / chemical synthesis*
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Isatin / chemistry
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / chemistry
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
Substances
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Caspase Inhibitors
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Recombinant Proteins
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Sulfonamides
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Isatin
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CASP6 protein, human
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Caspase 3
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Caspase 6