Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).
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.
Bajusz
S
S
Institute for Drug Research, Budapest, Hungary. h13770baj@ella.hu
Fauszt
I
I
Németh
K
K
Barabás
E
E
Juhász
A
A
Patthy
M
M
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
D061945:Caspase Inhibitors; D015853:Cysteine Proteinase Inhibitors; D001224:Aspartic Acid; D020170:Caspase 1