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Literature summary for 3.4.22.61 extracted from

  • Watt, W.; Koeplinger, K.A.; Mildner, A.M.; Heinrikson, R.L.; Tomasselli, A.G.; Watenpaugh, K.D.
    The atomic-resolution structure of human caspase-8, a key activator of apoptosis (1999), Structure Fold. Des., 7, 1135-1143.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
crystallization of the enzyme covalently modified with acetyl-IETD-aldehyde, hanging- and sitting-drop vapor diffusion Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
acetyl-IETD-aldehyde IC50: 50 nM, covalently modifies the active site C360 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.066
-
acetyl-IETD-4-nitroanilide pH 7.5, 37°C Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
11000
-
alpha2beta2, 2 * 18000 + 2 * 11000, crystallographic data Homo sapiens
18000
-
alpha2beta2, 2 * 18000 + 2 * 11000, crystallographic data Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the initiator caspase-8 activates other downstream caspases that are incapable of autocatalytic processing and activation ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q14790
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-DEVD-4-nitroanilide + H2O
-
Homo sapiens acetyl-DEVD + 4-nitroaniline
-
?
acetyl-IETD-4-nitroanilide + H2O
-
Homo sapiens acetyl-IETD + 4-nitroaniline
-
?
additional information the catalytic triad in caspase-8 comprises C260, H317 and the backbone carbonyl oxygen atom of R258, which points towards the Nepsilon atom of H317 Homo sapiens ?
-
?
additional information the initiator caspase-8 activates other downstream caspases that are incapable of autocatalytic processing and activation Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
tetramer alpha2beta2, 2 * 18000 + 2 * 11000, crystallographic data Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005
-
IC50: 50 nM, covalently modifies the active site C360 Homo sapiens acetyl-IETD-aldehyde