BRENDA - Enzyme Database show
show all sequences of 1.10.5.1

Old and new inhibitors of quinone reductase 2

Ferry, G.; Hecht, S.; Berger, S.; Moulharat, N.; Coge, F.; Guillaumet, G.; Leclerc, V.; Yous, S.; Delagrange, P.; Boutin, J.A.; Chem. Biol. Interact. 186, 103-109 (2010)

Data extracted from this reference:

Cloned(Commentary)
Commentary
Organism
the His-tagged enzyme is expressed in the Sf9 Spodoptera frugiperda ovarian cell line ATCC CRL-1711
Homo sapiens
Inhibitors
Inhibitors
Commentary
Organism
Structure
chrysoeriol
-
Homo sapiens
Melatonin
QR2 is inhibited in the micromolar range by melatonin, but not when using N-benzyl dihydronicotinamide and coenzyme Q2 are used as substrates
Homo sapiens
additional information
dicoumarol is inactive up to 0.1 mM
Homo sapiens
resveratrol
-
Homo sapiens
S26695
i.e. N-[2-(7-methylaminosulfonyl-1-naphthyl)ethyl]acetamide
Homo sapiens
S29434
i.e. N-[2-(2-methoxy-6H-dipyrido[2,3-a:3,2-e]pyrrolizin-11-yl)ethyl]-2-furamide, inhibits QR2 activity with an IC50 in the low nanomolar range from 0.7 to 80 nM, depending on the substrates and co-substrates used
Homo sapiens
KM Value [mM]
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
0.0102
-
2,6-dichlorophenolindophenol
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0111
-
menadione
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0113
-
N-benzyl dihydronicotinamide
using menadione as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0137
-
coenzyme Q0
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0361
-
N-benzyl dihydronicotinamide
using coenzyme Q0 as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0387
-
coenzyme Q2
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0404
-
N-benzyl dihydronicotinamide
using 2,6-dichlorophenolindophenol as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0451
-
N-benzyl dihydronicotinamide
using coenzyme Q1 as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0517
-
coenzyme Q1
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0602
-
N-benzyl dihydronicotinamide
using coenzyme Q2 as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
Localization
Localization
Commentary
Organism
GeneOntology No.
Textmining
cytosol
-
Homo sapiens
5829
-
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
-
-
-
Purification (Commentary)
Commentary
Organism
Ni-NTA column chromatography
Homo sapiens
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
additional information
the enzyme does not accept conventional phosphorylated nicotinamides as hydride donors
711729
Homo sapiens
?
-
-
-
-
N-benzyldihydronicotinamide + 2,6-dichlorophenolindophenol
-
711729
Homo sapiens
N-benzylnicotinamide + reduced 2,6-dichlorophenolindophenol
-
-
-
?
N-benzyldihydronicotinamide + menadione
-
711729
Homo sapiens
N-benzylnicotinamide + menadiol
-
-
-
?
N-benzyldihydronicotinamide + oxidized coenzyme Q0
-
711729
Homo sapiens
N-benzylnicotinamide + reduced coenzyme Q20
-
-
-
?
N-benzyldihydronicotinamide + oxidized coenzyme Q1
-
711729
Homo sapiens
N-benzylnicointamide + reduced coenzyme Q1
-
-
-
?
N-benzyldihydronicotinamide + oxidized coenzyme Q2
-
711729
Homo sapiens
N-benzylnicotinamide + reduced coenzyme Q2
-
-
-
?
nicotinamide riboside + menadiol
-
711729
Homo sapiens
dihydronicotinamide riboside + menadione
-
-
-
?
nicotinamide riboside + reduced 2,6-dichlorophenolindophenol
-
711729
Homo sapiens
dihydronicotinamide riboside + 2,6-dichlorophenolindophenol
-
-
-
?
nicotinamide riboside + reduced coenzyme Q0
-
711729
Homo sapiens
dihydronicotinamide riboside + coenzyme Q0
-
-
-
?
nicotinamide riboside + reduced coenzyme Q1
-
711729
Homo sapiens
dihydronicotinamide riboside + coenzyme Q1
-
-
-
?
nicotinamide riboside + reduced coenzyme Q2
-
711729
Homo sapiens
dihydronicotinamide riboside + coenzyme Q2
-
-
-
?
Cofactor
Cofactor
Commentary
Organism
Structure
FAD
-
Homo sapiens
IC50 Value
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.0000007
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S29434
0.000005
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S29434
0.0000067
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S29434
0.000016
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
chrysoeriol
0.000076
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
chrysoeriol
0.000079
-
using N-benzyl dihydronicotinamide and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S29434
0.000129
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
resveratrol
0.000143
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
resveratrol
0.00016
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
chrysoeriol
0.00082
-
using N-benzyl dihydronicotinamide and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
chrysoeriol
0.0012
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S26695
0.0025
-
using N-benzyl dihydronicotinamide and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S26695
0.0028
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
Melatonin
0.0029
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
resveratrol
0.0126
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S26695
0.0151
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S26695
0.0397
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
Melatonin
0.0415
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
Melatonin
0.07
-
using N-benzyl dihydronicotinamide and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
resveratrol
Cloned(Commentary) (protein specific)
Commentary
Organism
the His-tagged enzyme is expressed in the Sf9 Spodoptera frugiperda ovarian cell line ATCC CRL-1711
Homo sapiens
Cofactor (protein specific)
Cofactor
Commentary
Organism
Structure
FAD
-
Homo sapiens
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.0000007
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S29434
0.000005
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S29434
0.0000067
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S29434
0.000016
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
chrysoeriol
0.000076
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
chrysoeriol
0.000079
-
using N-benzyl dihydronicotinamide and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S29434
0.000129
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
resveratrol
0.000143
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
resveratrol
0.00016
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
chrysoeriol
0.00082
-
using N-benzyl dihydronicotinamide and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
chrysoeriol
0.0012
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S26695
0.0025
-
using N-benzyl dihydronicotinamide and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S26695
0.0028
-
using nicotinamide riboside and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
Melatonin
0.0029
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
resveratrol
0.0126
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S26695
0.0151
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
S26695
0.0397
-
using nicotinamide riboside and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
Melatonin
0.0415
-
using N-benzyl dihydronicotinamide and menadione as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
Melatonin
0.07
-
using N-benzyl dihydronicotinamide and coenzyme Q2 as substrates, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
resveratrol
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
chrysoeriol
-
Homo sapiens
Melatonin
QR2 is inhibited in the micromolar range by melatonin, but not when using N-benzyl dihydronicotinamide and coenzyme Q2 are used as substrates
Homo sapiens
additional information
dicoumarol is inactive up to 0.1 mM
Homo sapiens
resveratrol
-
Homo sapiens
S26695
i.e. N-[2-(7-methylaminosulfonyl-1-naphthyl)ethyl]acetamide
Homo sapiens
S29434
i.e. N-[2-(2-methoxy-6H-dipyrido[2,3-a:3,2-e]pyrrolizin-11-yl)ethyl]-2-furamide, inhibits QR2 activity with an IC50 in the low nanomolar range from 0.7 to 80 nM, depending on the substrates and co-substrates used
Homo sapiens
KM Value [mM] (protein specific)
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
0.0102
-
2,6-dichlorophenolindophenol
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0111
-
menadione
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0113
-
N-benzyl dihydronicotinamide
using menadione as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0137
-
coenzyme Q0
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0361
-
N-benzyl dihydronicotinamide
using coenzyme Q0 as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0387
-
coenzyme Q2
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0404
-
N-benzyl dihydronicotinamide
using 2,6-dichlorophenolindophenol as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0451
-
N-benzyl dihydronicotinamide
using coenzyme Q1 as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0517
-
coenzyme Q1
using N-benzyl dihydronicotinamide as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
0.0602
-
N-benzyl dihydronicotinamide
using coenzyme Q2 as cosubstrate, at 25°C, in 50 mM Tris-HCl, pH 8.5
Homo sapiens
Localization (protein specific)
Localization
Commentary
Organism
GeneOntology No.
Textmining
cytosol
-
Homo sapiens
5829
-
Purification (Commentary) (protein specific)
Commentary
Organism
Ni-NTA column chromatography
Homo sapiens
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
additional information
the enzyme does not accept conventional phosphorylated nicotinamides as hydride donors
711729
Homo sapiens
?
-
-
-
-
N-benzyldihydronicotinamide + 2,6-dichlorophenolindophenol
-
711729
Homo sapiens
N-benzylnicotinamide + reduced 2,6-dichlorophenolindophenol
-
-
-
?
N-benzyldihydronicotinamide + menadione
-
711729
Homo sapiens
N-benzylnicotinamide + menadiol
-
-
-
?
N-benzyldihydronicotinamide + oxidized coenzyme Q0
-
711729
Homo sapiens
N-benzylnicotinamide + reduced coenzyme Q20
-
-
-
?
N-benzyldihydronicotinamide + oxidized coenzyme Q1
-
711729
Homo sapiens
N-benzylnicointamide + reduced coenzyme Q1
-
-
-
?
N-benzyldihydronicotinamide + oxidized coenzyme Q2
-
711729
Homo sapiens
N-benzylnicotinamide + reduced coenzyme Q2
-
-
-
?
nicotinamide riboside + menadiol
-
711729
Homo sapiens
dihydronicotinamide riboside + menadione
-
-
-
?
nicotinamide riboside + reduced 2,6-dichlorophenolindophenol
-
711729
Homo sapiens
dihydronicotinamide riboside + 2,6-dichlorophenolindophenol
-
-
-
?
nicotinamide riboside + reduced coenzyme Q0
-
711729
Homo sapiens
dihydronicotinamide riboside + coenzyme Q0
-
-
-
?
nicotinamide riboside + reduced coenzyme Q1
-
711729
Homo sapiens
dihydronicotinamide riboside + coenzyme Q1
-
-
-
?
nicotinamide riboside + reduced coenzyme Q2
-
711729
Homo sapiens
dihydronicotinamide riboside + coenzyme Q2
-
-
-
?
Other publictions for EC 1.10.5.1
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
742815
Riches
The ontogeny and population v ...
Homo sapiens
J. Biochem. Mol. Toxicol.
31
0000
2017
-
-
-
-
-
-
1
-
1
-
-
1
-
2
-
-
-
-
-
2
-
-
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
1
-
-
-
-
-
2
-
-
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
724559
John
Design, synthesis, biological ...
Homo sapiens
Bioorg. Med. Chem.
21
6022-6037
2013
-
-
1
1
-
-
34
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
2
-
1
-
-
-
1
-
-
-
1
-
-
-
-
1
-
1
-
-
-
34
1
1
-
-
-
-
-
-
-
1
-
-
-
-
2
-
1
-
-
-
1
-
-
-
-
1
1
-
-
-
725512
Leung
Chloroquine binding reveals fl ...
Homo sapiens
J. Biol. Chem.
288
11242-11251
2013
-
-
-
1
-
-
2
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
1
-
-
-
2
-
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-
-
-
-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
725158
Antoine
-
Characterization of cofactors, ...
Homo sapiens
Int. J. Mass Spectrom.
312
87-96
2012
-
-
1
-
-
-
4
-
1
-
-
1
-
1
-
-
-
-
-
1
-
-
2
1
1
-
-
-
1
-
-
1
-
-
-
-
-
1
1
-
-
-
-
4
-
-
1
-
-
1
-
-
-
-
-
1
-
-
2
1
1
-
-
-
1
-
-
-
-
2
2
-
-
-
725669
Michaelis
Dabigatran and dabigatran ethy ...
Homo sapiens
J. Med. Chem.
55
3934-3944
2012
-
-
-
-
-
-
17
-
-
-
-
2
-
1
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
1
3
-
2
-
-
-
1
-
-
-
2
17
3
-
-
-
-
2
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
724751
Dufour
Mechanism-based inhibition of ...
Homo sapiens
ChemBioChem
12
1203-1208
2011
-
-
-
-
-
-
12
-
-
-
-
1
-
2
-
-
-
-
-
-
-
-
1
1
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
12
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
725071
Reybier
Insights into the redox cycle ...
Homo sapiens
Free Radic. Res.
45
1184-1195
2011
-
-
1
-
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2
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7
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10
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