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Literature summary for 3.4.25.1 extracted from

  • Zhang, X.; Frezza, M.; Milacic, V.; Ronconi, L.; Fan, Y.; Bi, C.; Fregona, D.; Dou, Q.P.
    Inhibition of tumor proteasome activity by gold-dithiocarbamato complexes via both redox-dependent and -independent processes (2010), J. Cell. Biochem., 109, 162-172.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
additional information gold(I)- and gold(III)-compound-mediated proteasome inhibition and cell death induction are completely reversed by the addition of reducing agents, e.g. dithiothreitol or N-acetyl-L-cysteine Homo sapiens
additional information gold(I)- and gold(III)-compound-mediated proteasome inhibition and cell death induction are completely reversed by the addition of reducing agents, e.g. dithiothreitol or N-acetyl-L-cysteine Oryctolagus cuniculus
[Au(ESDT)]2 i.e. AUL15, a gold(I)-dithiocarbamato species, inhibits the chymotrypsin-like activity of purified 20S proteasome and 26S proteasome in breast cancer cells Homo sapiens
[Au(ESDT)]2 i.e. AUL15, a gold(I)-dithiocarbamato species, inhibits the chymotrypsin-like activity of purified 20S proteasome Oryctolagus cuniculus
[AuBr2(ESDT)] i.e. AUL12, a gold(III)-dithiocarbamato species, inhibits the chymotrypsin-like activity of purified 20S proteasome and 26S proteasome in breast cancer cells Homo sapiens
[AuBr2(ESDT)] i.e. AUL12, a gold(III)-dithiocarbamato species, inhibits the chymotrypsin-like activity of purified 20S proteasome Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Oryctolagus cuniculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation purified 20S proteasome Oryctolagus cuniculus
-
MDA-MB-231 cell breast cancer cells 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 Oryctolagus cuniculus N-succinyl-LLVY + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
20S proteasome
-
Homo sapiens
20S proteasome
-
Oryctolagus cuniculus
26S proteasome
-
Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Oryctolagus cuniculus

General Information

General Information Comment Organism
additional information inhibition of the proteasomes by gold complexes results in accumulation of ubiquitinated proteins and proteasome target proteins, and induction of cell death, but at significantly different levels Homo sapiens