Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.19.12 extracted from

  • Mitsui, T.; Hirayama, K.; Aoki, S.; Nishikawa, K.; Uchida, K.; Matsumoto, T.; Kabuta, T.; Wada, K.
    Identification of a novel chemical potentiator and inhibitors of UCH-L1 by in silico drug screening (2010), Neurochem. Int., 56, 679-686.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
ethyl 1-[N-(4-methylphenyl)-N-(methylsulfonyl)alanyl]-4-piperidinecarboxylate
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(1,3-benzodioxol-5-ylmethyl)-4-(4-([(4-chlorophenyl)thio]methyl)benzoyl) piperazine slight inhibition of UCH-L1 Homo sapiens
2-([4-(2-furylmethyl)-5-(2-thienylmethyl)-4H-1,2,4-triazol-3-yl]thio)-N-(2-methoxydibenzo[b,d]furan-3-yl)acetamide
-
Homo sapiens
2-[(5-ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio]-N-(4-methyl-2-pyridinyl)acetamide
-
Homo sapiens
4-([benzyl(methyl)amino]sulfonyl)-N-[5-(benzylthio)-1,3,4-thiadiazol-2-yl]benzamide
-
Homo sapiens
8-[(1H-benzimidazol-2-ylmethyl)sulfanyl]-2,2-dimethyl-5-(morpholin-4-yl)-1,4-dihydro-2H-pyrano[4'',3'':4',5']pyrido[3',2':4,5]thieno[3,2-d]pyrimidine
-
Homo sapiens
additional information kinetics and inhibitor docking study using crystal structure data of PDB code 2ETL, overview. No or poor inhibition by 3-methyl-8-(4-methyl-1-piperazinyl)-7-(3-phenylpropyl)-3,7-dihydro-1Hpurine-2,6-dione, 1-(4-methoxyphenyl)-4-([3-(4-methoxyphenyl)-1,2,4-oxadiazol-5-yl]methyl)piperazine, N1-cyclopropyl-N2-(4-ethoxyphenyl)-N2-[(4-methylphenyl)sulfonyl]glycinamide, N-[6-((2-[(4-chlorophenyl)thio]acetyl)amino)-1,3-benzothiazol-2-yl]butanamide and N-1,3-benzothiazol-2-yl-2-([5-(4-morpholinylmethyl)-4-phenyl-4H-1,2,4-triazol-3-yl]thio)acetamide Homo sapiens
N,N'-(oxydi-4,1-phenylene)dibenzenesulfonamide slight inhibition of UCH-L1 Homo sapiens
N,N'-4,4'-biphenyldiylbis(4-ethylbenzenesulfonamide) strong inhibition of UCH-L1 Homo sapiens
N-(2-[(6,7-dimethoxy-1-isoquinolinyl)methyl]-4,5-dimethoxyphenyl)-4-(2-oxo-1-pyrrolidinyl)benzenesulfonamide slight inhibition of UCH-L1 Homo sapiens
N-(3,6-dichloro-2-pyridinyl)-N'-([(4,6-diphenyl-2-pyrimidinyl)amino]carbonyl)sulfamide
-
Homo sapiens
N-(4-([(4-ethoxyphenyl)amino]sulfonyl)phenyl)-2-naphthalenesulfonamide slight inhibition of UCH-L1 Homo sapiens
N-(4-([(4-methylphenyl)amino]sulfonyl)phenyl)-2-phenyl-2-(phenylthio)acetamide slight inhibition of UCH-L1 Homo sapiens
N-[2-(4-benzyl-1-piperazinyl)-2-oxoethyl]-N-(3-methylphenyl)benzenesulfonamide slight inhibition of UCH-L1 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09936
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant UCH-L1 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ubiquitin-4-methylcoumarine 7-amide + H2O
-
Homo sapiens ubiquitin + 7-amino-4-methylcoumarine
-
?

Synonyms

Synonyms Comment Organism
ubiquitin-C-terminal hydrolase L1
-
Homo sapiens
UCH-L1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.8
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.015
-
-
Homo sapiens N,N'-4,4'-biphenyldiylbis(4-ethylbenzenesulfonamide)

General Information

General Information Comment Organism
malfunction the hydrolase activity of UCH-L1 is implicated in Alzheimer's disease and cancer invasion Homo sapiens