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Literature summary extracted from

  • Frydrych, I.; Mlejnek, P.
    Serine protease inhibitors N-alpha-tosyl-L-lysinyl-chloromethylketone (TLCK) and N-tosyl-L-phenylalaninyl-chloromethylketone (TPCK) do not inhibit caspase-3 and caspase-7 processing in cells exposed to pro-apoptotic inducing stimuli (2008), J. Cell. Biochem., 105, 1501-1506.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.22.60 N6-(2-isopentenyl)adenosine highly induces enzyme activation Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.56 Ac-DEVD-CHO a caspase-3 inhibitor Homo sapiens
3.4.22.56 additional information processing of caspase-3 is affected only negligibly in cells treated with etoposide or N6-(2-isopentenyl)adenosine Homo sapiens
3.4.22.56 N-alpha-tosyl-L-lysinyl-chloromethylketone TLCK, a serine protease inhibitor and potent but nonspecific inhibitor of mature caspases, TLCK has no or only slight effect on caspase-3 processing, but TLCK substantially inhibits caspase-3 enzymatic DEVDase activity, but does not prevent cells from death Homo sapiens
3.4.22.56 N-tosyl-L-phenylalaninyl-chloromethylketone TPCK, a serine protease inhibitor and potent but nonspecific inhibitor of mature caspases, enhances caspase-3 processing although it substantially inhibits caspase-3 enzymatic DEVDase activity in HL-60 cells exposed to various cell death inducing stimuli, but does not prevent cells from death, overview Homo sapiens
3.4.22.60 N-alpha-tosyl-L-lysyl-chloromethylketone i.e. TLCK, substantially inhibits caspase-7 enzymatic DEVDase activity, but does not affect caspase-7 processing in cells exposed to pro-apoptotic inducing stimuli, irreversibly alkylates cysteine residues of the active site of cysteine proteases Homo sapiens
3.4.22.60 N-tosyl-L-phenylalanyl-chloromethylketone i.e. TPCK, enhances caspase-7 processing although it substantially inhibits caspase-7 enzymatic DEVDase activity in HL-60 cells exposed to various cell death inducing stimuli, irreversibly alkylates cysteine residues of the active site of cysteine proteases Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.22.60 additional information Homo sapiens inhibition of executioner caspase enzymatic activity by TLCK and TPCK in dying HL-60 cells is important in prevention of cell death ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.56 Homo sapiens
-
-
-
3.4.22.60 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.56 HL-60 cell
-
 Homo sapiens
-
3.4.22.60 HL-60 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.56 Ac-DEVD-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Ac-DEVD + 7-amino-4-methylcoumarin
-
 ?
3.4.22.60 Ac-Asp-Glu-Val-Asp-7-amido-4-methylcoumarin + H2O a caspase-3 substrate Homo sapiens Ac-Asp-Glu-Val-Asp + 7-amino-4-methylcoumarin
-
 ?
3.4.22.60 additional information inhibition of executioner caspase enzymatic activity by TLCK and TPCK in dying HL-60 cells is important in prevention of cell death Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.56 DEVDase
-
 Homo sapiens
3.4.22.60 DEVDase
-
 Homo sapiens