Conformationally constrained inhibitors of caspase-1 (interleukin-1β converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, APOPAIN)

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 19, 1998, Pages 2757-2762

  Karanewsky, Donald S ^a   Bai, Xu ^a   Linton, Steven D ^a   Krebs, Joseph F ^a   Wu, Joe ^a   Pham, Bryan ^a   Tomaselli, Kevin J ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CASPASE 3; CASPASE INHIBITOR; CPP 32; ENZYME INHIBITOR; INTERLEUKIN 1BETA CONVERTING ENZYME; UNCLASSIFIED DRUG;

APOPTOSIS; ARTICLE; CELL DEATH; CRYSTAL STRUCTURE; CRYSTALLIZATION; ENZYME CONFORMATION; ENZYME INHIBITION; HYDROGEN BOND; MEDIATOR RELEASE; MOLECULAR RECOGNITION; NONHUMAN;

CASPASE 1; CASPASE 3; CASPASES; CYSTEINE PROTEINASE INHIBITORS; DIPEPTIDES; HUMANS; MOLECULAR CONFORMATION; OLIGOPEPTIDES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0032491247     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00498-3     Document Type: Article

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33. 15. Fluorescence enzyme assays utilizing recombinant mICE and hCPP32 enzymes were carried out essentially according to Thornberry (ref 1c) and Nicholson (ref 4c), respectively. The substrate is Ac-Try ValAlaAsp-(7-amino-4-methylcoumarin) for the mICE assay and Ac-AspGluValAsp-(7-amino-4-methylcoumarin) for the hCPP32 assay. Enzyme reactions were run in ICE buffer (25 mM HEPES, 1 mM EDTA, 0.1% CHAPS, 10% sucrose, pH 7.5) containing 2 mM DTT at room temperature in duplicate.