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Literature summary for 3.4.25.1 extracted from

  • Baldisserotto, A.; Destro, F.; Vertuani, G.; Marastoni, M.; Gavioli, R.; Tomatis, R.
    N-terminal-prolonged vinyl ester-based peptides as selective proteasome beta1 subunit inhibitors (2009), Bioorg. Med. Chem., 17, 5535-5540.
    View publication on PubMed
Search for more literature for 3.4.25.1

Inhibitors

Inhibitors Comment Organism Structure
epoxomicin
-
 Homo sapiens
MG132
-
 Homo sapiens
additional information screening of compounds for in vitro capacity to inhibit the chymotryptic-, tryptic-like, and post-acidic activities of the proteasome, overview. Detection of N-terminal-prolonged vinyl ester-based peptides as selective proteasome beta1 subunit inhibitors. The inhibitors demonstrate resistance to plasmatic proteases and a good capacity to permeate the cell membrane, but low inhibitory potencies. Inhibitors of the post-acidic activity of proteasomes neither induce cell death nor greatly inhibit cell proliferation Homo sapiens
Z-b-Ala-Val-Ser-Leu-vinyl ester
-
 Homo sapiens
Z-beta-Ala-Leu-Leu-Leu-vinyl ester
-
 Homo sapiens
Z-Gly-Leu-Leu-Leu-vinyl ester
-
 Homo sapiens
Z-Gly-Val-Ser-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)3-CO-Leu-Leu-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)3-CO-Val-Ser-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)4-CO-Leu-Leu-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)4-CO-Val-Ser-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)5-CO-Leu-Leu-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)5-CO-Val-Ser-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)6-CO-Leu-Leu-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)6-CO-Val-Ser-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)7-CO-Leu-Leu-Leu-vinyl ester
-
 Homo sapiens
Z-NH-(CH2)7-CO-Val-Ser-Leu-vinyl ester
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
lymphoblastoid cell line
-
 Homo sapiens
-
mononuclear cell from peripheral blood Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzoyl-LRR-4-methyl-7-amido-coumarin + H2O trypsin-like proteasome activity Homo sapiens benzoyl-LRR + 4-methyl-7-amino-coumarin
-
 ?
N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O chymotrypsin-like proteasome activity Homo sapiens N-succinyl-LLVY + 7-amino-4-methylcoumarin
-
 ?
Z-LLE-4-methyl-7-amido-coumarin + H2O post-acidic proteasome activity Homo sapiens Z-LLE + 4-methyl-7-amino-coumarin
-
 ?

Synonyms

Synonyms Comment Organism
multi-subunit protease complex
-
 Homo sapiens
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 barrel-shaped proteolytic 20S proteasome core particle which consists of four seven-subunit rings, is capped at one or both ends by 19S regulatory particles and is the central part of the large, 2.4 MDa, multi-subunit protease complexes performing ATP-dependent degradation of poly-ubiquitinated proteins, and being responsible for the majority of the non-lysosomal proteolysis which occurs in eukaryotic cells Homo sapiens