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Literature summary for 3.4.22.61 extracted from

  • Abe, A.; Yamada, H.
    Harmol induces apoptosis by caspase-8 activation independently on Fas/Fas ligand interaction in human lung carcinoma H596 cells (2009), Anticancer Drugs, 20, 373-381.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
harmol i.e. 1-methyl-9H-beta-carbolin-7-ol, a natural beta-carboline plant alkaloid, induces caspase-8 activation Homo sapiens
additional information no enzyme activation by natural beta-carboline alkaloids harmalol, harmine, and harmaline, i.e. 1-methyl-4,9-dihydro-3H-beta-carbolin-7-ol, 7-methoxy-1-methyl-9H-beta-carboline, and 7-methoxy-1-methyl-4,9-dihydro-3H-beta-carboline, respectively Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
benzyloxycarbonyl-LEHD-fluoromethylketone a caspase-9 inhibitor, partial inhibition of caspase-8 activation in lung carcinoma cells Homo sapiens
N-carbobenzyloxy-IETD-fluoromethyl ketone a caspase-8 inhibitor, inhibition of caspase-8 activation in lung carcinoma cells Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens harmol activates caspase-8 to 334% and induces apoptosis by caspase-8 activation independently on Fas/Fas ligand interaction in human lung carcinoma H-596 cells, but not in H-596, H-226, and A-549 cells ?
-
?
procaspase-3 + H2O Homo sapiens activation of effector caspase-3 by the initiator caspase-8 caspase-3 + ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
lung carcinoma cell
-
Homo sapiens
-
NCI-H596 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-IETD-7-amido-4-fluoromethylcoumarin + H2O
-
Homo sapiens acetyl-IETD + 7-amino-4-fluoromethylcoumarin
-
?
additional information harmol activates caspase-8 to 334% and induces apoptosis by caspase-8 activation independently on Fas/Fas ligand interaction in human lung carcinoma H-596 cells, but not in H-596, H-226, and A-549 cells Homo sapiens ?
-
?
procaspase-3 + H2O activation Homo sapiens caspase-3 + ?
-
?
procaspase-3 + H2O activation of effector caspase-3 by the initiator caspase-8 Homo sapiens caspase-3 + ?
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens