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Literature summary extracted from

  • Huo, C.; Yang, H.; Cui, Q.C.; Dou, Q.P.; Chan, T.H.
    Proteasome inhibition in human breast cancer cells with high catechol-O-methyltransferase activity by green tea polyphenol EGCG analogs (2010), Bioorg. Med. Chem., 18, 1252-1258.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.6 (-)-epigallocatechin-3-O-gallate
-
 Homo sapiens
2.1.1.6 (2R,3R)-5,7-bis(acetyloxy)-2-[3,4,5-tris(acetyloxy)phenyl]-3,4-dihydro-2H-chromen-3-yl 3,4-bis(acetyloxy)-5-(2-oxopropyl)benzoate
-
 Homo sapiens
2.1.1.6 (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-trihydroxybenzoate)
-
 Homo sapiens
2.1.1.6 (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-dihydroxybenzoate)
-
 Homo sapiens
2.1.1.6 (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis[3,4,5-tris(acetyloxy)benzoate]
-
 Homo sapiens
2.1.1.6 (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis[3,5-bis(acetyloxy)benzoate]
-
 Homo sapiens
2.1.1.6 additional information (-)-epigallocatechin is not active even at a concentration of 0.05 mM Homo sapiens
3.4.25.1 (-)-epigallocatechin-3-gallate i.e. EGCG, inhibits the proteasomal chymotrypsin-like activity Homo sapiens
3.4.25.1 (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-triethoxybenzoate) inhibits 48% of MDA-MB-231 cell proliferation at 0.05 mM Homo sapiens
3.4.25.1 (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-trihydroxybenzoate)
-
 Homo sapiens
3.4.25.1 (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-diethoxybenzoate) 70-79% inhibition in MDA-MB-231 cells at 0.025-0.050 mM Homo sapiens
3.4.25.1 (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-dihydroxybenzoate)
-
 Homo sapiens
3.4.25.1 additional information inhibition of purified 20S proteasome and 26S proteasome activities by epigallocatechin-3-gallate and its analogues, overview Homo sapiens
3.4.25.1 pro-epigallocatechin-3-gallate i.e. pro-EGCG, inhibitory efficacy is greatly improved from 42% inhibition to 89% inhibition when combined with 3,5-dinitrocatechol Homo sapiens

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.6 breast cancer cell
-
 Homo sapiens
-
2.1.1.6 MDA-MB-231 cell
-
 Homo sapiens
-
3.4.25.1 MDA-MB-231 cell breast cancer cell Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.6 (-)-epigallocatechin-3-O-gallate + S-adenosyl-L-methionine
-
 Homo sapiens S-adenosyl-L-homocysteine + ?
-
 ?
3.4.25.1 N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O chymotrypsin-like proteasome activity Homo sapiens N-succinyl-LLVY + 7-amino-4-methylcoumarin
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.1.1.6 COMT
-
 Homo sapiens
3.4.25.1 20S proteasome
-
 Homo sapiens
3.4.25.1 proteasome
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.25.1 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.25.1 7.5
-
 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.1.1.6 0.029
-
 70-79% inhibition at 0.025-0.05 mM Homo sapiens (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-dihydroxybenzoate)
3.4.25.1 0.000086 0.000194 inhibition of the chymotrypsin-like activity of the proteasome in vitro, pH not specified in the publication, temperature not specified in the publication Homo sapiens (-)-epigallocatechin-3-gallate
3.4.25.1 0.019
-
 for the chymotrypsin-like activity, pH 7.5, 37°C Homo sapiens (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-trihydroxybenzoate)
3.4.25.1 0.029
-
 for the chymotrypsin-like activity, pH 7.5, 37°C Homo sapiens (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-dihydroxybenzoate)