A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety

ChemMedChem

Volumn 5, Issue 5, 2010, Pages 730-738

  Boxer, Matthew B ^a   Quinn, Amy M ^a   Shen, Min ^a   Jadhav, Ajit ^a   Leister, William ^a   Simeonov, Anton ^a   Auld, Douglas S ^a   Thomas, Craig J ^a  

^a NATIONAL HUMAN GENOME RESEARCH INSTITUTE   (United States)

Author keywords

Caspases; Covalent modifiers; Cysteine proteases; Inhibitors; VRT 043198; VX 765

Indexed keywords

1 [2 (4 AMINO 3 CHLOROBENZAMIDO) 3,3 DIMETHYLBUTANOYL] N [1 CYANO 2 (1H TETRAZOL 5 YL)ETHYL]PYRROLIDINE 2 CARBOXAMIDE; 3 [1 [2 (4 AMINO 3 CHLOROBENZAMIDO) 3,3 DIMETHYLBUTANOY]PYRROLIDINE 2 CARBOXAMIDO] 3 CYANOPROPANOIC ACID; 3 CYANOPROPIONIC ACID; CASPASE; CYSTEINE; ELECTROPHILE; ETHYL 3 [1 [2 (4 AMINO 3 CHLOROBENZAMIDO) 3,3 DIMETHYLBUTANOYL]PYRROLIDINE 2 CARBOXAMIDO] 3 CYANOPROPANOATE; INTERLEUKIN 1BETA CONVERTING ENZYME; INTERLEUKIN 1BETA CONVERTING ENZYME INHIBITOR; NCGC 00183434; NCGC 00183681; NCGC 00185682; NITRILE; PRODRUG; PROPIONIC ACID DERIVATIVE; UNCLASSIFIED DRUG; VRT 043198; VX 765;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DOWN REGULATION; DRUG HYDROLYSIS; DRUG POTENCY; DRUG SELECTIVITY; DRUG STABILITY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; IN VIVO STUDY; NONHUMAN; PRIORITY JOURNAL; RAT;

4-AMINOBENZOIC ACID; ANIMALS; BINDING SITES; CASPASE 1; CATALYTIC DOMAIN; COMPUTER SIMULATION; CYSTEINE PROTEINASE INHIBITORS; DIPEPTIDES; HUMANS; MICROSOMES, LIVER; PROPIONIC ACIDS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77951683942     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.200900531     Document Type: Article

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