title: Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).
abstract: Inhibition of interleukin-1 beta converting enzyme (ICE), apopain, papain, thrombin and trypsin with substrate like peptidyl L- and D-alpha-aldehydes and their L-beta-homo-aldehyde analogues was investigated. The L-beta-homo-aspartals appear to be specific inhibitors for ICE and its homologues; the other enzymes were not inhibited with such L-beta-homo aldehydes. Papain shows tolerance for D-residues at P1 depending on their chiral stability.
authors.affiliation: Institute for Drug Research, Budapest, Hungary. h13770baj@ella.hu
authors.forename: S
authors.initials: S
authors.lastname: Bajusz
authors.forename: I
authors.initials: I
authors.lastname: Fauszt
authors.forename: K
authors.initials: K
authors.lastname: Németh
authors.forename: E
authors.initials: E
authors.lastname: Barabás
authors.forename: A
authors.initials: A
authors.lastname: Juhász
authors.forename: M
authors.initials: M
authors.lastname: Patthy
mesh_terms: D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology*; D020170:Caspase 1 / Q000378:metabolism; D061945:Caspase Inhibitors; D015853:Cysteine Proteinase Inhibitors / Q000494:pharmacology*; D006801:Humans; D013379:Substrate Specificity
chemical_list: D061945:Caspase Inhibitors; D015853:Cysteine Proteinase Inhibitors; D001224:Aspartic Acid; D020170:Caspase 1