3.4.19.12: ubiquitinyl hydrolase 1

This is an abbreviated version, for detailed information about ubiquitinyl hydrolase 1, go to the full flat file.

Reaction

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) =

Synonyms

A20, AD-019, AMSH, associated molecule with the SH3-domain of STAM, AT-3, ataxin-3, BAP1, BPLF1, BRCA1-associated protein-1, C-terminal hydrolases UCHL3, C-terminal ubiquitin hydrolase, Cezanne, CGI-70, CYLD, de-ubiquitinating enzyme, deubiquinating isopeptidase T, deubiquitinating enzyme, Doa4, Doa4 ubiquitin hydrolase, Doa4p ubiquitin isopeptidase, DUB, dUCH, esterase, ubiquitin thiol-, hydrolase, ubiquitin carboxyl-terminal, hydrolase, ubiquitin carboxyl-terminal (Aplysia californica gene Ap-uch), Iso-T, isopeptidase, isopeptidase T, More, Neuron cytoplasmic protein 9.5, neuronal-specific protein gene product 9.5, OTU-1, ovarian tumour 1, PA-700 associated isopeptidase, papain-like protease, PGP 9.5, PGP 9.5/UCHL1, PGP9.5, PGP9.5.1, PLpro, Ub isopeptidase, ubiquitin C terminal hydrolase 1, ubiquitin C-terminal hydrolase, ubiquitin C-terminal hydrolase (Aplysia californica gene Ap-uch), ubiquitin C-terminal hydrolase 1, ubiquitin C-terminal hydrolase 37, ubiquitin C-terminal hydrolase 8, ubiquitin C-terminal hydrolase isoform L3, ubiquitin C-terminal hydrolase L-1, ubiquitin C-terminal hydrolase L1, ubiquitin C-terminal hydrolase L3, Ubiquitin C-terminal hydrolase UCH37, ubiquitin C-terminal hydrolase-1, ubiquitin C-terminal hydrolase-L1, ubiquitin C-terminal hydrolase-L3, ubiquitin C-terminal hydrolase-L5, ubiquitin C-terminal hydrorase-L1, ubiquitin carboxy terminal hydrolase-L1, ubiquitin carboxy terminal hydrolase-L3, ubiquitin carboxy-terminal hydrolase, ubiquitin carboxy-terminal hydrolase 1, ubiquitin carboxy-terminal hydrolase L1, ubiquitin carboxy-terminal hydrolase-L1, ubiquitin carboxy-terminal hydrolase-L3, ubiquitin carboxyhydrolase L3, ubiquitin carboxyl terminal esterase L1, ubiquitin carboxyl terminal hydrolase 1, ubiquitin carboxyl terminal hydrolase L1, ubiquitin carboxyl-terminal hydrolase, ubiquitin carboxyl-terminal hydrolase 1, ubiquitin carboxyl-terminal hydrolase 44, ubiquitin carboxyl-terminal hydrolase isozyme L1, ubiquitin carboxyl-terminal hydrolase L-1, ubiquitin carboxyl-terminal hydrolase L1, ubiquitin carboxyl-terminal hydrolase l3, ubiquitin carboxyl-terminal hydrolase L5, ubiquitin carboxyl-terminal hydrolase-L1, ubiquitin carboxyterminal hydrolase L1, ubiquitin carboxyterminal hydrolase L3, ubiquitin carboxyterminal hydrolase-L1, ubiquitin hydrolase, ubiquitin hydrolase Uch-L1, ubiquitin hydrolase UCH-L3, ubiquitin isopeptidase, Ubiquitin thiolesterase, Ubiquitin thiolesterase L1, Ubiquitin thiolesterase L3, Ubiquitin thiolesterase L4, Ubiquitin thiolesterase L5, ubiquitin-C-terminal hydrolase L1, ubiquitin-carboxyl-terminal hydrolase PGP-9.5, ubiquitin-specific protease 44, UBPY, UCH, UCH L-1, UCH L1, UCH-1, UCH-8, UCH-L1, UCH-L2, UCH-L3, UCH-L4, UCH-L5, UCH37, UCH54, UCHL-1, UCHL-3, UCHL1, UCHL1/PGP 9.5, UCHL2, Uchl3, UCHL5, UCHL5N240, USP19, USP22, USP44, yeast ubiquitin hydrolase, YUH, YUH1

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.19 Omega peptidases
                3.4.19.12 ubiquitinyl hydrolase 1

Inhibitors

Inhibitors on EC 3.4.19.12 - ubiquitinyl hydrolase 1

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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
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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
RNAi
-
siRNA
-
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
-