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Literature summary for 3.4.22.56 extracted from

  • Tawa, P.; Giroux, A.; Grimm, E.; Han, Y.; Nicholson, D.W.; Xanthoudakis, S.
    Correlating the fractional inhibition of caspase-3 in NT2 cells with apoptotic markers using an active-caspase-3 enzyme-linked immunosorbent assay (2006), Anal. Biochem., 350, 32-40.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
C143A inactive enzyme. Catalytically inactive p17 polypeptide is expressed in a stable manner, while wild-type p17 is rapidly degraded Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3S)-3-[(2-[3-[(N-acetyl-L-alpha-aspartyl)amino]-2-oxopyridin-1(2H)-yl]butanoyl)amino]-5-(benzylsulfanyl)-4-oxopentanoic acid 50% inhibition at 52 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer Homo sapiens
(3S)-3-[(2-[3-[(N-acetyl-L-alpha-aspartyl)amino]-2-oxopyridin-1(2H)-yl]butanoyl)amino]-5-[(2-chloro-6-fluorobenzyl)sulfanyl]-4-oxopentanoic acid 50% inhibition at 0.3 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer Homo sapiens
(3S)-5-(benzylsulfanyl)-3-([N-[(2,5-dimethoxyphenyl)acetyl]-L-valyl]amino)-4-oxopentanoic acid 50% inhibition at 48 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer Homo sapiens
(3S)-5-(benzylsulfanyl)-3-[(N-[[2-ethoxy-5-(2-methoxy-2-oxoethoxy)phenyl]acetyl]-L-valyl)amino]-4-oxopentanoic acid 50% inhibition at 86 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer Homo sapiens
(3S)-5-[(2-chloro-6-fluorobenzyl)sulfanyl]-3-[(N-[[2-ethoxy-5-(2-methoxy-2-oxoethoxy)phenyl]acetyl]-L-valyl)amino]-4-oxopentanoic acid 50% inhibition at 53 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer Homo sapiens
N-acetyl-L-alpha-aspartyl-L-alanyl-N-[(1S)-1-(carboxymethyl)-2-oxo-5-phenylpentyl]-L-valinamide 50% inhibition at 2 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer Homo sapiens
N-acetyl-L-alpha-aspartyl-L-alanyl-N-[(1S)-3-(benzylsulfanyl)-1-(carboxymethyl)-2-oxopropyl]-L-valinamide 50% inhibition at 0.5 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer Homo sapiens
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-N-[(1S)-2-carboxy-1-formylethyl]-L-valinamide 50% inhibition at 27 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell generation of enzyme from latent proenzyme dimer upon induction of apoptosis Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-DEVD-7-amido-4-methylcoumarin + H2O
-
Homo sapiens acetyl-DEVD + 7-amino-4-methylcoumarin
-
?

Subunits

Subunits Comment Organism
heterotetramer 2 * p17, large subunit, + 2 * p12, small subunit, SDS-PAGE Homo sapiens