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Literature summary for 3.4.25.1 extracted from

  • Sun, Q.; Xu, B.; Niu, Y.; Xu, F.; Liang, L.; Wang, C.; Yu, J.; Yan, G.; Wang, W.; Jin, H.; Xu, P.
    Synthesis, bioactivity, docking and molecular dynamics studies of furan-based peptides as 20S proteasome inhibitors (2015), ChemMedChem, 10, 498-510.
    View publication on PubMed
Search for more literature for 3.4.25.1

Inhibitors

Inhibitors Comment Organism Structure
bortezomib
-
 Homo sapiens
carfilzomib
-
 Homo sapiens
marizomib
-
 Homo sapiens
MG-132
-
 Homo sapiens
N-(tert-butoxycarbonyl)-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide 60.06% inhibition at 0.01 mM Homo sapiens
N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide 89.7% inhibition at 0.01 mM Homo sapiens
N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide 69.7% inhibition at 0.01 mM Homo sapiens
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide 58.5% inhibition at 0.01 mM Homo sapiens
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide 73.4% inhibition at 0.01 mM Homo sapiens
N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide 82.2% inhibition at 0.01 mM Homo sapiens
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide 7.7% inhibition at 0.01 mM Homo sapiens
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide 16.5% inhibition at 0.01 mM Homo sapiens
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-O-methyl-L-tyrosinamide 73% inhibition at 0.01 mM Homo sapiens
Nalpha-[(2S)-2-[2-(tert-butoxycarbonyl)hydrazinyl]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
 Homo sapiens
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-(4-methoxyphenyl)butanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide 84.8% inhibition at 0.01 mM Homo sapiens
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide 47.5% inhibition at 0.01 mM Homo sapiens
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide 67.1% inhibition at 0.01 mM Homo sapiens
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide 14.9% inhibition at 0.01 mM Homo sapiens
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide 5.7% inhibition at 0.01 mM Homo sapiens
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide 13.6% inhibition at 0.01 mM Homo sapiens
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-O-methyl-L-tyrosinamide 60.5% inhibition at 0.01 mM Homo sapiens
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide 36.4% inhibition at 0.01 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-375 cell
-
 Homo sapiens
-
A-549 cell
-
 Homo sapiens
-
BGC-823 cell
-
 Homo sapiens
-
DU-145 cell
-
 Homo sapiens
-
HCT-8 cell
-
 Homo sapiens
-
HeLa cell
-
 Homo sapiens
-
Hep-G2 cell
-
 Homo sapiens
-
HL-60 cell
-
 Homo sapiens
-
JURKAT cell
-
 Homo sapiens
-
MCF-7 cell
-
 Homo sapiens
-
SW-480 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-succinyl-LLVY-aminoluciferin + H2O
-
 Homo sapiens ?
-
 ?
Z-LRR-aminoluciferin + H2O
-
 Homo sapiens ?
-
 ?
Z-nLPnLD-aminoluciferin + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
20S proteasome
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000373
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens MG-132
0.00164
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
0.00262
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
0.00327
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-(4-methoxyphenyl)butanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
0.00585
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
0.00601
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-O-methyl-L-tyrosinamide
0.00642
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
0.00682
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-O-methyl-L-tyrosinamide
0.00756
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
0.00785
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(2S)-2-[2-(tert-butoxycarbonyl)hydrazinyl]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
0.00815
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
0.00839
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
0.00942
-
 in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens N-(tert-butoxycarbonyl)-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
0.01
-
 IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
0.01
-
 IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
0.01
-
 IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
0.01
-
 IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
0.01
-
 IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
0.01
-
 IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C Homo sapiens Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide