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5.3.4.1: protein disulfide-isomerase

This is an abbreviated version!
For detailed information about protein disulfide-isomerase, go to the full flat file.

Word Map on EC 5.3.4.1

Reaction

catalyses the rearrangement of -S-S- bonds in proteins =

Synonyms

5'-MD, 58 kDa glucose regulated protein, 58 kDa microsomal protein, AGR2, anterior gradient homolog 2, BPA-binding protein, CaBP1, CaBP2, Cellular thyroid hormone binding protein, cotyledon-specific chloroplast biogenesis factor CYO1, CYO1, DbsG, disulfide bond isomerase, disulfide bond-forming enzyme, Disulfide interchange enzyme, disulfide isomerase, Disulfide isomerase ER-60, disulfide-bond isomerase, dithiol-disulfide isomerase, Dsb, DsbA, DsbB, DsbC, DsbD, DsbG, ECaSt/PDI, endoplasmic reticulum protein EUG1, Eps1p, ER protein 57, ER58, ER60, ERcalcistorin/protein-disulfide isomerase, ERdj5, Ero1, Erp, ERP-57, ERp-72 homolog, ERp18, ERp27, ERp28, ERp44, Erp46, ERp5, ERp57, ERP59, ERP60, ERp72, Eug1p, fibronectin, gPDI-1, gPDI-2, gPDI-3, HIP-70, HlPDI-1, HlPDI-2, HlPDI-3, Iodothyronine 5'-monodeiodinase, More, Mpd1p, Mpd2p, multifunctional protein disulfide isomerase, ncgl2478, P5, P55, P58, pancreas-specific protein disulfide isomerase, PDI, PDI A4, PDI I, PDI II, pdi-15, PDI-1a, pdi-40, pdi-47, pdi-52, PDI-A, PDI-M, PDI-P5, PDI-related protein, PDI1, PDI11, PDI2, PDI7, PDI8, PDIA1, PDIA2, PDIA3, PDIA4, PDIA6, PDIL-1, PDIL-2, PDIL1-1, PDIL1;1, PDIL1Aalpha, PDIL1B, PDIL2, PDIL2-3, PDIL3A, PDIL4D, PDIL5A, PDILT, PDIp, PDIr, protein disulfide isomerase, protein disulfide isomerase 1, protein disulfide isomerase 2, protein disulfide isomerase 3, protein disulfide isomerase A1, protein disulfide isomerase A3, protein disulfide isomerase A5, protein disulfide isomerase A6, protein disulfide isomerase associated 3, Protein disulfide isomerase P5, protein disulfide isomerase-1, protein disulfide isomerase-11, protein disulfide isomerase-2, protein disulfide isomerase-3, protein disulfide isomerase-8, protein disulfide isomerase-like protein of the testis, protein disulfide isomerase-P5, protein disulfide isomerase-related chaperone Wind, Protein disulfide isomerase-related protein, protein disulfide oxidoreductase, protein disulfide reductase/isomerase, protein disulfide-isomerase A4, Protein disulphide isomerase, Protein ERp-72, protein-disulfide isomerase, R-cognin, RB60, Rearrangease, Reduced ribonuclease reactivating enzyme, Retina cognin, S-S rearrangase, SSO0192, SsPDO, thiol-disulfide oxidoreductase, thiol-protein oxidoreductase, thioredoxin domain-containing protein 5, Thyroid hormone-binding protein, Thyroxine deiodinase, TXNDC5, yPDI

ECTree

     5 Isomerases
         5.3 Intramolecular oxidoreductases
             5.3.4 Transposing S-S bonds
                5.3.4.1 protein disulfide-isomerase

Inhibitors

Inhibitors on EC 5.3.4.1 - protein disulfide-isomerase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,1-bis(4-hydroxyphenyl)ethane
-
i.e.bisphenol E, 15% inhibition at 0.0125 mM
1,3-diphenylpropane
-
8% inhibition at 0.0125 mM
12-O-Tetradecanoylphorbol 13-acetate
-
binds to and moderately inhibits PDI
16F16
-
irreversible inhibition
2',3,3',4',5'-pentachlorobiphenyl
-
strong inhibition of PDI 3,3',5-triiodo-L-thyronine-binding activity
2',3,3',5,5',6'-hexachlorobiphenyl
-
strong inhibition of PDI 3,3',5-triiodo-L-thyronine-binding activity
2,2-bis(4-hydroxyphenyl)propane
-
i.e. bisphenol A, 30% inhibition at 0.0125 mM
2,4-dinitrochlorobenzene
-
2-(2-carboxy-4-nitro-phenyl) disulfonyl-5-nitrobenzoic acid
i.e. NSC517871. Molecular docking simulation into the redox-active site, residues C37, G38, H39, C40. Inhibitor binds to hydrophobic amino acidsA34, W36, C37, C40, H39, T68 and F80. The redox inhibitory conformations are energetically and statistically favored
2-nitro-5-sulfo-sulfonyl-benzoic acid
molecular docking simulation into the redox-active site, residues C37, G38, H39, C40. Inhibitor binds to hydrophobic amino acidsA34, W36, C37, C40, H39, T68 and F80. The redox inhibitory conformations are energetically and statistically favored
2-Nitro-5-thiocyanobenzoic acid
molecular docking simulation into the redox-active site, residues C37, G38, H39, C40. Inhibitor binds to hydrophobic amino acidsA34, W36, C37, C40, H39, T68 and F80. The redox inhibitory conformations are energetically and statistically favored
2-[[4-(cyclopropanecarbonyl)piperazin-1-yl]methyl]-1,2-benzothiazol-3(2H)-one
-
potent, reversible inhibition
3,3',5-triiodo-L-thyronine
3,3',5-triiodothyronine
-
-
3,4-dichlorophenol
4,4'-diisothiocyano-2,2'-stilbene disulfonic acid
-
considerably more effective after preincubation with DTT
4,4'-methylenebisphenol
-
12% inhibition at 0.0125 mM
4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol
-
-
4-alpha-cumylphenol
-
18% inhibition at 0.0125 mM
4-amino-phenylarsine oxide
-
0.0058 mM, 50% inhibition of tyramine-S-S-poly(D-lysine) reduction
4-chloromercuribenzoic acid
4-hydroxy-2-nonenal
-
44% inhibition at 0.03 mM
4-nonylphenol
4-octylphenol
5,5'-dithiobis(2-nitrobenzoic acid)
-
0.0049 mM, 50% inhibition of tyramine-S-S-poly(D-lysine) reduction
5-(3-carboxy-4-nitro-phenyl) sulfonyl-2-nitrobenzoic acid
i.e. NSC695265. Molecular docking simulation into the redox-active site, residues C37, G38, H39, C40. Inhibitor binds to hydrophobic amino acidsA34, W36, C37, C40, H39, T68 and F80. The redox inhibitory conformations are energetically and statistically favored
8-azido-ATP
-
for the ATPase activity, binds at the same site as ATP
acrolein
-
79% inhibition at 0.03 mM
anti-PDI Fab fragments
-
-
-
AsO43-
-
-
bacitracin
bacitracin A
bacitracin B
-
-
bacitracin F
-
-
bacitracin H
-
-
bisphenol A
Ca2+
-
1 mM, 40% inhibition
CCF642
-
-
-
cumene hydroperoxide
-
deoxycholate
-
-
Diazobenzene sulfonic acid
-
considerably more effective after preincubation with DTT
Dithionitrobenzoic acid
molecular docking simulation into the redox-active site, residues C37, G38, H39, C40. Inhibitor binds to hydrophobic amino acidsA34, W36, C37, C40, H39, T68 and F80. The redox inhibitory conformations are energetically and statistically favored
dithiothreitol
-
treatment decreases the content of 52 kDa isoform by half
E-64
-
0.01 mM, 11% inhibition after treatment with 0.01 mM DTT. No inhibition without DTT
Estrogens
-
-
-
ethyl N-[[[(cyanocarbonyl)(2,4-dimethoxyphenyl)amino]thiophen-2-yl]acetyl]glycinate
-
-
genistein
-
suppresses binding of proinsulin to PDI, inhibits 66% of PDIs chaperone activity
gentamycin
-
analysis of binding and dissociation constants with PDI and PDI domain deletion mutants
iodoacetamide
iodoacetate
isoquercetin
-
-
kanamycin
-
analysis of binding and dissociation constants with PDI and PDI domain deletion mutants
LOC14
-
-
MA3 018
-
inhibition of protein disulfide isomerase. Treatment of Mn2+-treated endothelial cells abolishes the conversion of integrin alphaVbeta to the ligand-competent high-affinity state
-
MA3 019
-
inhibition of protein disulfide isomerase. Treatment of Mn2+-treated endothelial cells abolishes the conversion of integrin alphaVbeta to the ligand-competent high-affinity state
-
methyl-methanethiosulfonate
-
abolishes PDI oxidoreductase but not chaperone activity
Mg2+
-
1 mM, 20% inhibition
N-acetylated-triiodothyronine
-
0.07 mM, 50% inhibition of tyramine-S-S-poly(D-lysine) reduction
N-ethylmaleimide
N-Iodoacetyl-N'-(5-sulfo)-1-naphthyl-diaminoethane
-
incubation after pretreatment with DTT or GSH
N-[2-methyl-2-(morpholin-4-yl)propyl]-1,2-benzothiazol-3-amine
-
-
NEM
-
incubation after pretreatment with DTT or GSH
neomycin
-
analysis of binding and dissociation constants with PDI and PDI domain deletion mutants
nitazoxanide
-
a broad-spectrum anti-parasitic drug
nitazoxanide thiazolide derivatives
-
PDI is inhibited by those thiazolides that also affected parasite proliferation
-
paromomycin
-
analysis of binding and dissociation constants with PDI and PDI domain deletion mutants
Pentachlorophenol
peptides
-
study of the inhibition of enzyme catalyzed reduction of insulin by GSH by peptides of various length and amino acid composition
phenyl vinyl sulfonate
-
-
Phenylarsine oxide
-
complete inhibition at 0.01-0.1 mM in vivo
protein DS61
-
-
-
quercetin 3-rutinoside
-
-
quercetin-3-rutinoside
ribostamycin
S-nitrosocysteine
-
S-nitrosates endogenous or overexpressed PDI in HEK-293T cells
sisomycin
-
analysis of binding and dissociation constants with PDI and PDI domain deletion mutants
sodium hypochlorite
-
Somatostatin
-
streptomycin
-
analysis of binding and dissociation constants with PDI and PDI domain deletion mutants
tert-2-hexenal
-
32% inhibition at 1 mM
-
tetrabromobisphenyl A
tetrachlorobisphenyl A
thionitrobenzoic acid
molecular docking simulation into the redox-active site, residues C37, G38, H39, C40. Inhibitor binds to hydrophobic amino acidsA34, W36, C37, C40, H39, T68 and F80. The redox inhibitory conformations are energetically and statistically favored
tizoxanide
-
deacetylated metabolite of nitazoxanide
tocinoic acid
-
-
Vancomycin
-
analysis of binding and dissociation constants with PDI and PDI domain deletion mutants
vincristine
-
inhibits chaperone activity but not isomerase activity of both isoforms PDI and P5 in vitro. A 100:1 molar ratio of vincristine to enzyme is sufficient to almost completely inhibit chaperone activity
zinc bacitracin
specific inhibition; specific inhibition; specific inhibition
Zn2+
-
1 mM, 70% inhibition
additional information
-