Abstract
A systematic study of interleukin-1 beta converting enzyme (ICE, caspase-1) and caspase-3 (CPP32, apopain) inhibitors incorporating a P2-P3 conformationally constrained dipeptide mimetic is reported. Depending on the nature of the P4 substituent, highly selective inhibitors of both Csp-1 or Csp-3 were obtained.
MeSH terms
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Caspase 3
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Caspase Inhibitors*
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Cysteine Proteinase Inhibitors / chemical synthesis*
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Cysteine Proteinase Inhibitors / chemistry
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Cysteine Proteinase Inhibitors / pharmacology*
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Dipeptides / chemical synthesis
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Dipeptides / chemistry
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Dipeptides / pharmacology
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Humans
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Molecular Conformation
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Structure-Activity Relationship
Substances
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Caspase Inhibitors
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Cysteine Proteinase Inhibitors
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Dipeptides
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Oligopeptides
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CASP3 protein, human
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Caspase 3