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Literature summary extracted from

  • Rut, W.; Poreba, M.; Kasperkiewicz, P.; Snipas, S.J.; Drag, M.
    Selective substrates and activity-based probes for imaging of the human constitutive 20S proteasome in cells and blood samples (2018), J. Med. Chem., 61, 5222-5234 .
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.25.1 analysis simultaneous labeling and detection of constitutive 20S proteasome subunits using an affinity-based probe cocktail and application to biological samples Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.25.1 bortezomib
-
 Homo sapiens
3.4.25.1 MG-132
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.25.1 0.0094
-
 acetyl-Arg-hSer-Thr-Arg-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 0.0159
-
 acetyl-hArg-Pro-2-fluoro-Phe-Asp-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 0.0432
-
 acetyl-hArg-Pro-Abu-Asp-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 0.051
-
 acetyl-betaAla-Met(sulfone)-Thr-Arg-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.25.1 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.25.1 erythrocyte
-
 Homo sapiens
-
3.4.25.1 HEK-293F cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.25.1 acetyl-Arg-hSer-Thr-Arg-7-amido-4-methylcoumarin + H2O substrate for trypsin-like activity Homo sapiens acetyl-Arg-hSer-Thr-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.25.1 acetyl-betaAla-Met(sulfone)-Thr-Arg-7-amido-4-methylcoumarin + H2O substrate for trypsin-like activity Homo sapiens acetyl-betaAla-Met(sulfone)-Thr-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.25.1 acetyl-hArg-Pro-2-fluoro-Phe-Asp-7-amido-4-methylcoumarin + H2O substrate for caspase-like activity Homo sapiens acetyl-hArg-Pro-2-fluoro-Phe-Asp + 7-amino-4-methylcoumarin
-
 ?
3.4.25.1 acetyl-hArg-Pro-Abu-Asp-7-amido-4-methylcoumarin + H2O substrate for caspase-like activity Homo sapiens acetyl-hArg-Pro-Abu-Asp + 7-amino-4-methylcoumarin
-
 ?
3.4.25.1 acetyl-Phe-Thr(Bzl)-His(3-benzyloxymethyl)-Leu-7-amido-4-methylcoumarin + H2O substrate for chymotrypsin-like activity Homo sapiens acetyl-Phe-Thr(Bzl)-His(3-benzyloxymethyl)-Leu + 7-amino-4-methylcoumarin
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.25.1 1.343
-
 acetyl-hArg-Pro-Abu-Asp-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 1.844
-
 acetyl-hArg-Pro-2-fluoro-Phe-Asp-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 2.233
-
 acetyl-betaAla-Met(sulfone)-Thr-Arg-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 2.837
-
 acetyl-Arg-hSer-Thr-Arg-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.4.25.1 20.61
-
 acetyl-Phe-Thr(Bzl)-His(3-benzyloxymethyl)-Leu-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 31.11
-
 acetyl-hArg-Pro-Abu-Asp-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 43.79
-
 acetyl-betaAla-Met(sulfone)-Thr-Arg-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 116.1
-
 acetyl-hArg-Pro-2-fluoro-Phe-Asp-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.25.1 301
-
 acetyl-Arg-hSer-Thr-Arg-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens