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Literature summary for 3.4.22.62 extracted from

  • Sadhukhan, R.; Leone, J.W.; Lull, J.; Wang, Z.; Kletzien, R.F.; Heinrikson, R.L.; Tomasselli, A.G.
    An efficient method to express and refold a truncated human procaspase-9: a caspase with activity toward Glu-X bonds (2006), Protein Expr. Purif., 46, 299-308.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
DELTA1-111 a truncated form of procaspase-9 missing the first 111 amino acids, and a variety of mutants derived therefrom are expressed in Echerichia coli inclusion bodies. Upon refolding to active enzyme, DELTA1-111 procaspase-9 and mutants are recovered at purity greater than 95% with a final yield of 20-35 mg/L cell culture. the active procaspaseretains its prosegment, while undergoing major auto processing at ASp315 and a minor cleavage at Glu306 Homo sapiens
DELTA1-111/DELTAA316-D330 activity with acetyl-LEHD-7-amido-4-trifluoromethylcoumarin is 6fold higher than the activity of mutant DELTA1-111 Homo sapiens
DELTA1-111/DELTAA316-D330 activity with acetyl-LEHD-7-amido-4-trifluoromethyl coumarin is 6fold higher than the activity of mutant DELTA1-111 Homo sapiens
DELTA1-111/E306A/D315A E306A/D315A mutation blocks autoprocessing and shifts pH optimum from pH 6.2 for DELTA1-111 to pH 7.2. Activity with acetyl-LEHD-7-amido-4-trifluoromethyl coumarin is identical to the activity of mutant DELTA1-111 Homo sapiens
DELTA1-111/E306D/D315A activity with acetyl-LEHD-7-amido-4-trifluoromethylcoumarin is 90% of the activity of mutant DELTA1-111 Homo sapiens
DELTA1-111/E306D/D315A activity with acetyl-LEHD-7-amido-4-trifluoromethyl coumarin is 90% of the activity of mutant DELTA1-111 Homo sapiens
DELTA1-111/E306D/DELTAA316-D330 activity with acetyl-LEHD-7-amido-4-trifluoromethylcoumarin is 7.6fold higher than the activity of mutant DELTA1-111 Homo sapiens
DELTA1-111/E306D/DELTAA316-D330 activity with acetyl-LEHD-7-amido-4-trifluoromethyl coumarin is 7.6fold higher than the activity of mutant DELTA1-111 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
benzyloxycarbonyl-VAD-fluoromethylketone
-
Homo sapiens
benzyloxycarbonyl-VAE-fluoromethylketone
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
heart
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-LEHD-7-amido-4-trifluoromethyl coumarin + H2O
-
Homo sapiens acetyl-LEHD + 7-amino-4-trifluoromethyl coumarin
-
?
acetyl-LEHD-7-amido-4-trifluoromethylcoumarin + H2O
-
Homo sapiens acetyl-LEHD + 7-amino-4-trifluoromethylcoumarin
-
?

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.2
-
mutant DELTA1-111 Homo sapiens
7.2
-
mutant DELTA1-111/E306A/D315A Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0142
-
benzyloxycarbonyl-VAE-fluoromethylketone
-
Homo sapiens
0.0171
-
benzyloxycarbonyl-VAD-fluoromethylketone
-
Homo sapiens