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Literature summary for 3.4.25.1 extracted from

  • Baumann, P.; Mueller, K.; Mandl-Weber, S.; Leban, J.; Doblhofer, R.; Ammendola, A.; Baumgartner, R.; Oduncu, F.; Schmidmaier, R.
    The peptide-semicarbazone S-2209, a representative of a new class of proteasome inhibitors, induces apoptosis and cell growth arrest in multiple myeloma cells (2009), Br. J. Haematol., 144, 875-886.
    View publication on PubMed
Search for more literature for 3.4.25.1

Inhibitors

Inhibitors Comment Organism Structure
1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol) i.e. S-2209, potently inhibits chymotrypsin-like proteasome activity of the human 20S proteasome. S-2209 targets NFkappaB activity, overview. S-2209 inhibits cell growth and induces apoptosis in human multiple myeloma cells, mechanisms, overview Homo sapiens
1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol) i.e. S-2209, targets NFkappaB activity, overview Rattus norvegicus
bortezomib induces apoptosis in primary myeloma cells, but causes no induction of apoptosis in peripheral blood mononuclear cells from healthy humans Homo sapiens
bortezomib
-
 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
mononuclear cell peripheral blood Rattus norvegicus
-
myeloma cell primary, multiple Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O chymotrypsin-like proteasome activity Homo sapiens N-succinyl-LLVY + 7-amino-4-methylcoumarin
-
 ?
N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O chymotrypsin-like proteasome activity Rattus norvegicus N-succinyl-LLVY + 7-amino-4-methylcoumarin
-
 ?
succinyl-LLVY-aminoluciferin + H2O chymotrypsin-like proteasome activity Homo sapiens succinyl-LLVY + aminoluciferin
-
 ?
succinyl-LLVY-aminoluciferin + H2O chymotrypsin-like proteasome activity Rattus norvegicus succinyl-LLVY + aminoluciferin
-
 ?

Synonyms

Synonyms Comment Organism
20S proteasome
-
 Homo sapiens
20S proteasome
-
 Rattus norvegicus
proteasome
-
 Homo sapiens
proteasome
-
 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Homo sapiens
37
-
 assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens
7.5
-
 assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00022
-
 pH 7.5, 30°C Homo sapiens 1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol)