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Literature summary for 3.4.25.1 extracted from

  • Hindo, S.S.; Frezza, M.; Tomco, D.; Heeg, M.J.; Hryhorczuk, L.; McGarvey, B.R.; Dou, Q.P.; Verani, C.N.
    Metals in anticancer therapy: copper(II) complexes as inhibitors of the 20S proteasome (2009), Eur. J. Med. Chem., 44, 4353-4361.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.25.1

Inhibitors

Inhibitors Comment Organism Structure
(acetato-kappaO)[2,4-diiodo-6-({[(pyridin-2-yl-kappaN)methyl]amino-kappaN}methyl)phenolato-kappaO]copper a copper complex, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells Homo sapiens
chloro[2,4-diiodo-6-({[(pyridin-2-yl-kappaN)methyl]amino-kappaN}methyl)phenolato-kappaO]copper a copper complex, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells Homo sapiens
additional information assignment of species [CuLI]+ as the minimal pharmacophore needed for proteasomal chymotryspin-like activity inhibition, copper complex synthesis and structures, overview. The proteasomal chymotrypsin-like activity is inhibited by 45%, 60%,70% and 80% after 2, 4, 8, and 18 h, respectively, by the copper complexes in C4-2B prostate cancer cells, overview Homo sapiens
[Cu(HLI)(LI)]OAc a copper complex, HLI is the ligand 2,4-diiodo-6-((pyridine-2-ylmethylamino)methyl)phenol, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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-
-

Source Tissue

Source Tissue Comment Organism Textmining
LNCAP-C4-2B cell prostate cancer cell line Homo sapiens
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MCF-10A cell
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 Homo sapiens
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PC-3 cell prostate cancer cell line 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
-
 ?

Synonyms

Synonyms Comment Organism
20S proteasome
-
 Homo sapiens

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
7.5
-
 assay at Homo sapiens

General Information

General Information Comment Organism
additional information the proteasomal chymotrypsin-like activity inhibition is associated with accumulated levels of ubiquitinated proteins Homo sapiens