Information on EC 3.4.19.12 - ubiquitinyl hydrolase 1

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
3.4.19.12
-
RECOMMENDED NAME
GeneOntology No.
ubiquitinyl hydrolase 1
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Thiol-dependent hydrolysis of ester, thioester, amide, peptide and isopeptide bonds formed by the C-terminal Gly of ubiquitin (a 76-residue protein attached to proteins as an intracellular targeting signal)
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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-
-
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CAS REGISTRY NUMBER
COMMENTARY hide
189642-63-5
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86480-67-3
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
strain N2, Bristol
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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UniProt
Manually annotated by BRENDA team
strain Rafinesque, NWAC103, gene UCHL5
UniProt
Manually annotated by BRENDA team
strain Rafinesque, NWAC103, gene UCHL5
UniProt
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
; gene uchl1
UniProt
Manually annotated by BRENDA team
Mus musculus C57BL/6J
C57BL/6J mice
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-
Manually annotated by BRENDA team
DBA/2 mice
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-
Manually annotated by BRENDA team
ICR mice
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Manually annotated by BRENDA team
no activity in Escherichia coli
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Manually annotated by BRENDA team
3D7 strain
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
synthetic construct
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(His)8-Ub-CTAPIII + H2O
(His)8-Ub + CTAPII
show the reaction diagram
-
Ub i.e ubiquitin, CTAPII i.e. connective tissue-activating peptide
-
?
Ac-ALRGG-7-amido-4-trifluoromethylcoumarin
?
show the reaction diagram
Ac-LRGG-7-amido-4-trifluoromethylcoumarin
?
show the reaction diagram
Ac-RLRGG-7-amido-4-trifluoromethylcoumarin
?
show the reaction diagram
activity-based haemagglutinin-tagged ubiquitin + H2O
?
show the reaction diagram
-
-
-
-
?
alpha-Tubulin + H2O
?
show the reaction diagram
-
-
-
-
?
beta-tubulin + H2O
?
show the reaction diagram
-
-
-
-
?
branched di-ubiquitin + H2O
ubiquitin
show the reaction diagram
branched polyubiquitin + H2O
ubiquitin
show the reaction diagram
conjugate of histone H2A and ubiquitin + H2O
ubiquitin + histone H2A
show the reaction diagram
di-ubiquitin + H2O
ubiquitin
show the reaction diagram
EBV ribonucleotide reductase
?
show the reaction diagram
is deubiquitinated by BPLF1 1-246
-
-
?
HCF-1 + H2O
?
show the reaction diagram
HCF-1 is the principal Bap1-interacting protein. It is K48- and K63-ubiquitinated. Endogenous HCF-1C is ubiquitinated at lysine-1807 and/or lysine-1808
-
-
?
head-to-tail polyubiquitin + H2O
ubiquitin
show the reaction diagram
-
recombinant substrate from expression in Escherichia coli
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-
?
hemagglutinin-tagged ubiquitin-vinyl methyl ester + H2O
?
show the reaction diagram
-
-
-
-
?
inhibitor of kappa B-alpha + H2O
?
show the reaction diagram
-
UCHL1 deubiquitinates, thereby resulting in nuclear factor-kappa B inactivation
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-
?
K48-linked tetraubiquitin + H2O
K48-linked diubiquitin + diubiquitin
show the reaction diagram
-
-
-
-
?
K63-linked polyubiquitin + H2O
K63-linked polyubiquitin + ubiquitin
show the reaction diagram
-
-
-
-
?
linear ubiquitin-beta-galactosidase + H2O
ubiquitin + protein
show the reaction diagram
monoubiquitin + H2O
?
show the reaction diagram
N2-L-Asp-ubiquitin + H2O
ubiquitin + L-Asp
show the reaction diagram
-
-
-
?
N2-Lys-ubiquitin + H2O
ubiquitin + Lys
show the reaction diagram
-
ubiquitin amide of the alpha amino group of lysine
-
?
N6-(N2-acetyl)Lys-ubiquitin + H2O
ubiquitin + N2-acetyl-Lys
show the reaction diagram
-
ubiquitin amide of the alpha amino group of lysine
-
?
N6-Lys-ubiquitin + H2O
ubiquitin + Lys
show the reaction diagram
Nalpha-(diubiquitin)-[L-Lys] + H2O
?
show the reaction diagram
-
K48 linked diubiquitin
-
-
?
Nalpha-ubiquitin-[MQIFVRPR] + H2O
ubiquitin + MQIFVRPR
show the reaction diagram
-
-
-
-
?
Nedd-8 + H2O
?
show the reaction diagram
NEDD8-protein + H2O
NEDD8 + protein
show the reaction diagram
enzyme shows dual specificity for ubiquitin-conjugates and NEDD8-conjugates
-
?
Nepsilon-(diubiquitin)-[Nalpha-actyl-L-Lys] + H2O
?
show the reaction diagram
-
K48 linked diubiquitin
-
-
?
poly-His tagged di-ubiquitin + H2O
ubiquitin + ?
show the reaction diagram
-
-
-
-
?
polyubiquitin + H2O
ubiquitin
show the reaction diagram
Smad2 + H2O
?
show the reaction diagram
-
weaker association
-
-
?
Smad3 + H2O
?
show the reaction diagram
-
weaker association
-
-
?
Smad7 + H2O
?
show the reaction diagram
-
association with Smad7, which can act as an adaptor able to recruit UCH37 to the type I TGF-beta receptor and reverses Smurf-mediated ubiquitination
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-
?
spermidine-ubiquitin + H2O
ubiquitine + spermidine
show the reaction diagram
-
-
-
-
?
type I TGF-beta receptor + H2O
?
show the reaction diagram
ubiquitin + H2O
?
show the reaction diagram
ubiquitin + H2O
monoubiquitin
show the reaction diagram
-
UCH-L1 removes and recycles ubiquitin molecules from degraded proteins
-
-
?
ubiquitin 7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
ubiquitin C-terminal amide + H2O
ubiquitin + NH3
show the reaction diagram
-
-
-
-
?
ubiquitin C-terminal-4-methyl-7-amido-coumarin + H2O
ubiquitin + 4-methyl-7-amino-coumarin
show the reaction diagram
-
UCHL3 is 200fold more active than UCHL1/PGP 9.5
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-
?
ubiquitin ethyl ester + H2O
ubiquitin + ethanol
show the reaction diagram
ubiquitin ethylester + H2O
ubiquitin + an alcohol
show the reaction diagram
-
synthetic substrate
-
-
?
ubiquitin fused to 60% of its N-terminus + H2O
ubiquitin + 60% of ubiquitin N-terminus
show the reaction diagram
-
recombinant substrate, expressed in Escherichia coli
-
?
ubiquitin glycine methyl ester + H2O
ubiquitin + methanol
show the reaction diagram
-
-
-
-
?
ubiquitin metallothionein + H2O
?
show the reaction diagram
ubiquitin thiol ester of dithiothreitol + H2O
ubiquitin + dithiothreitol
show the reaction diagram
-
-
-
-
?
ubiquitin-4-methylcoumarin 7-amide + H2O
ubiquitin + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
ubiquitin-4-methylcoumarine 7-amide + H2O
ubiquitin + 7-amino-4-methylcoumarine
show the reaction diagram
-
-
-
-
?
ubiquitin-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-7-amido-4-methylcoumarin + H2O
ubiquitin + 7-amino-4-methylcoumarin
show the reaction diagram
ubiquitin-alcohol + H2O
ubiquitin + alcohol
show the reaction diagram
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-
-
ir
ubiquitin-alpha-NH-dihydrofolate reductase + H2O
ubiquitin + dihydrofolate reductase
show the reaction diagram
-
-
-
-
?
ubiquitin-alpha-NH-MHISPPEPESEEEEHYC + H2O
ubiquitin + MHISPPEPESEEEEHYC
show the reaction diagram
-
-
-
?
ubiquitin-alphaNH-MHISPPEPESEEEEHYC + H2O
ubiquitin + MHISPPEPESEEEEHYC
show the reaction diagram
ubiquitin-AMC
?
show the reaction diagram
BPLF1 1-246 expresses deubiquitinating activity, cleaves ubiquitin chains linked by K48 and K63
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-
?
ubiquitin-AMC + H2O
?
show the reaction diagram
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-
-
-
?
ubiquitin-AW + H2O
?
show the reaction diagram
ubiquitin-B domain of staphylococcal protein-A + H2O
ubiquitin + B domain of staphylococcal protein-A
show the reaction diagram
-
and variants thereof, substrate is expressed as alpha-linked C-terminal fusion to ubiquitin
-
-
?
ubiquitin-beta1 domain of streptococcal protein G + H2O
ubiquitin + beta1 domain of streptococcal protein G
show the reaction diagram
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and variants thereof, substrate is expressed as alpha-linked C-terminal fusion to ubiquitin
-
-
?
ubiquitin-carboxyl extension protein + H2O
ubiquitin + ubiquitin-carboxyl extension protein
show the reaction diagram
ubiquitin-CEP52 + H2O
ubiquitin + CEP52
show the reaction diagram
ubiquitin-CEP80 + H2O
ubiquitin + CEP80
show the reaction diagram
ubiquitin-Cys + H2O
ubiquitin + Cys
show the reaction diagram
-
-
-
?
ubiquitin-Cys-Cys + H2O
ubiquitin + Cys-Cys
show the reaction diagram
-
-
-
?
ubiquitin-Fur4p-conjugate + H2O
ubiquitin + Fur4p
show the reaction diagram
-
ubiquitin is bound to the Fur4p protein via its Lys63
-
?
ubiquitin-human carboxyl extension protein fusion protein + H2O
ubiquitin + human carboxyl extension protein
show the reaction diagram
ubiquitin-magainin + H2O
magainin + ubiquitin
show the reaction diagram
-
is efficiently cleaved at the carboxyl terminus of ubquitin, yielding recombinant magainin with high antimicrobial activity
-
-
?
ubiquitin-peptide + H2O
?
show the reaction diagram
ubiquitin-piscidin 1 + H2O
ubiquitin + piscidin 1
show the reaction diagram
-
-
-
?
ubiquitin-protein + H2O
ubiquitin + protein
show the reaction diagram
ubiquitin-rhodamine110-glycine + H2O
rhodamine110
show the reaction diagram
-
-
-
-
?
ubiquitin-W + H2O
?
show the reaction diagram
ubiquitin-W-G75A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-H68A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-I44A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-K11A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-K48A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-K63A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-K6A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-L71A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-L73A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-R42A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-R72A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-R74A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-W-V70A + H2O
?
show the reaction diagram
synthetic construct
-
-
-
-
?
ubiquitin-WA + H2O
?
show the reaction diagram
ubiquitinyl-7-amido-4-methylcoumarin + H2O
ubiquitin + 7-amino-4-methylcoumarin
show the reaction diagram
ubiquitinyl-peptide + H2O
ubiquitin + peptide
show the reaction diagram
ubiquitinyldihydrofolate reductase + H2O
ubiquitin + dihydrofolate reductase
show the reaction diagram
-
UCH-1
-
?
Z-Arg-Leu-Arg-Gly-Gly-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
polyubiquitin + H2O
ubiquitin
show the reaction diagram
type I TGF-beta receptor + H2O
?
show the reaction diagram
Q9Y5K5
UCH37 deubiquitinates and stabilizes type I TGF-beta receptor. Overexpression of UCH37 upregulates TGF-beta-dependent transcription
-
-
?
ubiquitin-CEP52 + H2O
ubiquitin + CEP52
show the reaction diagram
ubiquitin-CEP80 + H2O
ubiquitin + CEP80
show the reaction diagram
ubiquitin-peptide + H2O
?
show the reaction diagram
ubiquitin-protein + H2O
ubiquitin + protein
show the reaction diagram
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cu2+
-
0.2 mol per mol of protein, native isozyme ISOT-S
Divalent cations
Ni2+
-
0.5 mol per mol of protein, native isozyme ISOT-S
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(3E)-1-(3,4-dichlorobenzyl)-4-methoxy-5-phenyl-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0061 mM
(3E)-1-(3,4-dichlorobenzyl)-5-iodo-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.00094 mM; IC50: 0.016 mM
(3E)-1-(3,4-dichlorobenzyl)-5-methoxy-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0029 mM
(3E)-1-{2-bromo-2-[3-(trifluoromethyl)phenyl]ethyl}-5-chloro-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0095 mM
(3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carbonitrile
-
IC50: 0.012 mM
(3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carboxamide
-
IC50: 0.0041 mM
(3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carboxylic acid
-
IC50: 0.05 mM
(3E)-5-(trifluoromethoxy)-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0034 mM
(3E)-5-(trifluoromethoxy)-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime
-
IC50: 0.078 mM
(3E)-5-bromo-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.00081 mM
(3E)-5-chloro-1-(2,3-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0027 mM
(3E)-5-chloro-1-(2,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0012 mM
(3E)-5-chloro-1-(2,5-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.00088 mM
(3E)-5-chloro-1-(2-chloro-5-fluorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0065 mM
(3E)-5-chloro-1-(2-naphthylmethyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.014 mM
(3E)-5-chloro-1-(2-phenylethyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.019 mM
(3E)-5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0018 mM; IC50: 0.017 mM
(3E)-5-chloro-1-(3,5-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0013 mM
(3E)-5-chloro-1-(3-chloro-4-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.021 mM
(3E)-5-chloro-1-(3-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.013 mM
(3E)-5-chloro-1-(4-chlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.012 mM
(3E)-5-chloro-1-(4-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.052 mM
(3E)-5-chloro-1-[2-(3,4-dichlorophenoxy)ethyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0062 mM
(3E)-5-chloro-1-[2-(3,4-dichlorophenyl)ethyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0013 mM
(3E)-5-chloro-1-[2-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.018 mM
(3E)-5-chloro-1-[2-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime
-
IC50: 0.321 mM
(3E)-5-chloro-1-[3-(3,4-dichlorophenyl)propyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.016 mM
(3E)-5-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.006 mM; IC50: 0.036 mM
(3E)-5-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime
-
IC50: 0.114 mM
(3E)-5-chloro-1-[4-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.012 mM
(3E)-5-chloro-1-[4-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime
-
IC50: 0.013 mM
(3E)-5-chloro-1-{1-[2-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0088 mM
(3E)-5-chloro-1-{1-[2-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime
-
IC50: 0.045 mM
(3E)-5-chloro-1-{1-[3-(trichloromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0034 mM
(3E)-5-chloro-1-{1-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime
-
IC50: 0.022 mM
(3E)-5-chloro-1-{2-ethoxy-2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.095 mM
(3E)-5-chloro-1-{2-hydroxy-2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.019 mM
(3E)-5-chloro-1-{2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0041 mM
(3E)-5-chloro-1-{2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime
-
IC50: 0.08 mM
(3E)-5-chloro-7-methyl-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.012 mM
(3E)-5-fluoro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0061 mM
(3E)-5-fluoro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime
-
IC50: 0.043 mM
(3E)-6-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0058 mM
1-(1,3-benzodioxol-5-ylmethyl)-4-(4-([(4-chlorophenyl)thio]methyl)benzoyl) piperazine
-
slight inhibition of UCH-L1
1-benzyl-3-hydroxy-4-(5-methyl-2-furoyl)-5-(3-pyridinyl)-1,5-dihydro-2H-pyrrol-2-one
-
is a competitive inhibitor of UCH-L3, significantly inhibits hydrolysis activity of UCH-L3 by 83.2%
15-deoxy-DELTA12,14-prostaglandin J2
-
modification of UCH-L1 by cyclopentenone prostaglandins causes unfolding and aggregation. A single thiol group on Cys152 reacts with the alpha,beta-unsaturated carbonyl center in the cyclopentenone ring of prostaglandins, resulting in a covalent adduct, spectral analysis, overview
2-([4-(2-furylmethyl)-5-(2-thienylmethyl)-4H-1,2,4-triazol-3-yl]thio)-N-(2-methoxydibenzo[b,d]furan-3-yl)acetamide
-
-
2-propenal
-
carbonyl modification with 0.1 mM
2-[(5-ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio]-N-(4-methyl-2-pyridinyl)acetamide
-
-
3-amino-2-(4-methylbenzoyl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylaic acid
-
an uncompetitive inhibitor of UCHL1 that binds only to the Michaelis complex and not to free enzyme
3-amino-2-(cyclohexylcarbonyl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid
-
-
3-amino-2-keto-7Hthieno[2,3-b]pyridin-6-one derivative
-
-
3-amino-2-[(2-methoxyphenyl)carbonyl]-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid
-
-
3-amino-2-[(4-chlorophenyl)carbonyl]-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid
-
-
3-amino-2-[(4-methylphenyl)carbonyl]-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid
-
-
3-amino-2-[(4-tert-butylphenyl)carbonyl]-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid
-
-
3-amino-2-[(naphthalen-1-yloxy)carbonyl]-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid
-
-
3-amino-2-[(naphthalen-2-yloxy)carbonyl]-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid
-
-
3-amino-6-oxo-2-[[4-(trifluoromethyl)phenyl]carbonyl]-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylic acid
-
-
3-hydroxy-5-(4-methoxyphenyl)-1-(1,3,4-thiadiazol-2-yl)-4-(2-thienylcarbonyl)-1,5-dihydro-2H-pyrrol-2-one
-
significantly inhibits hydrolysis activity of UCH-L3 by 76.5%
3-[4-methyl-5-(([3-(2-thienyl)-1,2,4-oxadiazol-5-yl]methyl)thio)-4H-1,2,4-triazol-3-yl]-1H-indole
-
inhibits hydrolysis activity by 16.2%
4,5,6,7-tetrachloroindan-1,3-dione
-
UCH-L3 inhibition reduces epithelial sodium channel currents, decreases apical membrane epithelial sodium channel expression and increases epithelial sodium channel ubiquitination at the apical surface
4-([benzyl(methyl)amino]sulfonyl)-N-[5-(benzylthio)-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-hydroxy-2-hexenal
-
carbonyl modification in a dose-dependent manner
4-hydroxy-2-nonenal
-
carbonyl modification with 0.01-0.1 mM leads to decreased ubiquitin binding, and both increased insolubility and interactions with proteins over 30 kDa compared with the wild-type
5-(4-fluorophenyl)-3-hydroxy-4-(5-methyl-2-furoyl)-1-(3-pyridinylmethyl)-1,5-dihydro-2H-pyrrol-2-one
-
significantly inhibits hydrolysis activity of UCH-L3 by 76.8%
5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime)
-
IC50: 0.0018 mM
5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-oxime
-
IC50: 0.012 mM
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
-
-
aldehyde product of fatty acid peroxidation
i.e. HNE; modifies isozyme L1 at physiological concentrations of 0.01-0.1 mM and reduces enzyme activity, excess N-acetyl-L-cysteine protects
-
amyloid beta
-
30% inhibition
-
Antibody
-
anti-UCH antibodies increase the rate of polyspermy during in vitro fertilization by reducing UCH enzymatic activity
-
benzyloxycarbonyl-Val-Ala-Glu(gamma-methoxy) fluoromethylketone
-
co-crystal structure reveals that the inhibitor binds in the active-site cleft, irreversibly modifying the active-site cysteine
-
Ca2+
-
59% inhibition at 5 mM
dimethyl sulfoxide
-
catalytic activity decreases slightly with increasing dimethyl sulfoxide concentrations. At 2% (v/v) dimethyl sulfoxide, the proteolytic activity of UCH-L3 is reduced by ca. 5% in comparison to dimethyl sulfoxide-free conditions
dipicolinic acid
-
-
DTT
-
erythrocyte isozyme ISOT-S and ISOT-L, inhibition by chelating of Zn2+
EDTA
-
-
EGTA
-
-
epoxysuccinyl-leucylamido-(4-guanidino) butane
-
reduces UCH-L1 mRNA, protein level and activity. Caspase-mediated apoptosis in epoxysuccinyl-leucylamido-(4-guanidino) butane-treated fibroblasts is reversed by transfection with a UCH-L1 plasmid
iodoacetamide
isatin O-acyl oximes
-
reversible and competitive inhibition, inhibitory potency and features of the drivatives, specific inhibition of UCH-L1, poor inhibition of UCH-L3, IC50 values, overview
J series prostaglandins
-
inhibition of the enzyme is involved in disruption of the proteasome pathway and leads to apoptosis
-
KCl
-
92% inhibition at 0.2 M
LDN 57 444
-
UCH-L1 inhibition leads to a time and concentration-dependent formation of membrane protrusions, accompanied by redistribution of alpha-actinin-4 to the membrane. Expression level of alpha-actinin-4 remains stable, whereas the beta-catenin content increases. Inhibition of UCH-L1 does not induce apoptosis
LDN-57444
Mg2+
-
61% inhibition at 5 mM
N,N'-(oxydi-4,1-phenylene)dibenzenesulfonamide
-
slight inhibition of UCH-L1
N,N'-4,4'-biphenyldiylbis(4-ethylbenzenesulfonamide)
-
strong inhibition of UCH-L1
N-(2-[(6,7-dimethoxy-1-isoquinolinyl)methyl]-4,5-dimethoxyphenyl)-4-(2-oxo-1-pyrrolidinyl)benzenesulfonamide
-
slight inhibition of UCH-L1
N-(3,6-dichloro-2-pyridinyl)-N'-([(4,6-diphenyl-2-pyrimidinyl)amino]carbonyl)sulfamide
-
-
N-(4-([(4-ethoxyphenyl)amino]sulfonyl)phenyl)-2-naphthalenesulfonamide
-
slight inhibition of UCH-L1
N-(4-([(4-methylphenyl)amino]sulfonyl)phenyl)-2-phenyl-2-(phenylthio)acetamide
-
slight inhibition of UCH-L1
N-ethylmaleimide
N-[2-(4-benzyl-1-piperazinyl)-2-oxoethyl]-N-(3-methylphenyl)benzenesulfonamide
-
slight inhibition of UCH-L1
nitrilo-triacetate
-
-
oligomeric Abeta
-
treatment of hippocampal slices produces a deficit in long term potentiation. Effect can be reversed by coadministering a recombinant UCH-L1 protein
-
peptides
-
containing either of the cleavage site sequence found in ubiquitin polymers, but not unrelated peptides
tosyl-L-phenylalanine chloromethyl ketone
inhibits fragmentation of AT-3 carrying six consecutive glutamines
ubiquitin
Ubiquitin aldehyde
ubiquitin vinyl methyl ester
-
a ubiquitin-based suicide substrate, binding structure analysis with wild-type and mutant S18Y enzymes, overview
-
ubiquitin vinylmethyl ester
inhibitor forms a covalent adduct with the active site cysteine of the enzyme
-
ubiquitin vinylsulfone
-
irreversible inhibitor that covalently modifies the active-site cysteines of DUBs
-
ubiquitin-aldehyde
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-mercaptoethanol
4-hydroxy-2-alkenal
-
modification of UCH-L1 promotes direct interactions between UCH-L1 and tubulin
4-hydroxy-2-nonenal
-
modification of UCH-L1 promotes direct interactions between UCH-L1 and tubulin
Adrm1
-
recruits Uch37 to the proteasome. Binds the carboxy-terminal tail of Uch37. Following binding, Adrm1 relieves Uch37 autoinhibition, accelerating the hydrolysis of ubiquitin-7-amido-4-methylcoumarin
-
ethyl 1-[N-(4-methylphenyl)-N-(methylsulfonyl)alanyl]-4-piperidinecarboxylate
-
-
H2O2
-
-
poly-L-Arg
-
activation
poly-L-Lys
-
activation
Sodium citrate
activation of the enzymes with increasing salt concentration, reaching a maximum above 0.8 M. Most effective activation in the case of UCH-L3, where 1.1 M sodium citrate enhances catalysis on the synthetic substrate Ac-LRGG-7-amido-4-trifluoromethylcoumarin about 24fold, compared with low-salt conditions. The tetrapeptide substrate Ac-LRGG-7-amido-4-trifluoromethylcoumarin and the pentapeptide substrate containing alanine at position P5, namely Ac-ALRGG-7-amido-4-trifluoromethylcoumarin, both demonstrate a salt effect, but the pentapeptide substrate containing arginine in position P5, Ac-RLRGG-7-amido-4-trifluoromethylcoumarin, does not demonstrate one; activation of the enzymes with increasing salt concentration, reaching a maximum above 0.8 M. The tetrapeptide substrate Ac-LRGG-7-amido-4-trifluoromethylcoumarin and the pentapeptide substrate containing alanine at position P5, namely Ac-ALRGG-7-amido-4-trifluoromethylcoumarin, both demonstrate a salt effect, but the pentapeptide substrate containing arginine in position P5, Ac-RLRGG-7-amido-4-trifluoromethylcoumarin, does not demonstrate one; activation of the enzymes with increasing salt concentration, reaching a maximum above 0.8 M. Weakest activation in the case of IsoT, where there is almost no increase in catalysis compared with low salt conditions. The tetrapeptide substrate Ac-LRGG-7-amido-4-trifluoromethylcoumarin and the pentapeptide substrate containing alanine at position P5, namely Ac-ALRGG-7-amido-4-trifluoromethylcoumarin, both demonstrate a salt effect, but the pentapeptide substrate containing arginine in position P5, Ac-RLRGG-7-amido-4-trifluoromethylcoumarin, does not demonstrate one
TNFalpha
-
inducer
-
tumor necrosis factor-alpha
-
treatment of cultured vascular smooth muscle cells for 24 and 48 hours does not significantly alter UCHL1 mRNA levels, whereas long term treatment (96 hours) significantly increases UCHL1 mRNA levels. Treatment of aortic endothelial cells and aortic smooth muscle cells with tumor necrosis factor-alpha for 24 hours does not significantly alter UCHL1 mRNA levels
-
ubiquitin
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.002
branched dimeric ubiquitin
-
pH 7.2, 37C
-
0.015
head-to-tail dimeric ubiquitin
-
pH 7.2, 37C
-
0.000047 - 0.02149
ubiquitin 7-amido-4-methylcoumarin
0.0006 - 0.03
ubiquitin ethyl ester
0.0000833
ubiquitin-7-amido-4-methylcoumarin
-
-
-
0.00004 - 0.00016
ubiquitin-7-amino-4-methylcoumarin
0.00008
ubiquitin-AW
synthetic construct
-
with UCH-L1
-
0.000034
ubiquitin-rhodamine110-glycine
-
-
-
0.00013
ubiquitin-W
synthetic construct
-
with UCH-L1
-
0.0001 - 0.0004
ubiquitin-W-G75A
0.0011 - 0.002
ubiquitin-W-G76A
0.0005
ubiquitin-W-H68A
synthetic construct
-
with UCH-L1; with UCH-L3
-
0.00031 - 0.0004
ubiquitin-W-I44A
0.0011 - 0.0023
ubiquitin-W-K11A
0.0003 - 0.0007
ubiquitin-W-K48A
0.0004 - 0.0008
ubiquitin-W-K63A
0.0009 - 0.0014
ubiquitin-W-K6A
0.008 - 0.0198
ubiquitin-W-L71A
0.0058 - 0.0104
ubiquitin-W-L73A
0.0282 - 0.03
ubiquitin-W-L8A
0.0001
ubiquitin-W-R42A
synthetic construct
-
with UCH-L1; with UCH-L3
-
0.0006 - 0.0019
ubiquitin-W-R72A
0.0002 - 0.0045
ubiquitin-W-R74A
0.0006 - 0.0011
ubiquitin-W-V70A
0.00045
ubiquitin-WA
synthetic construct
-
with UCH-L1
-
0.000035 - 0.00016
ubiquitinyl-7-amido-4-methylcoumarin
0.0033
wild-type di-ubiquitin
-
pH 8.0, 37C
-
additional information
additional information