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(-)-epigallocatechin-3-gallate
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noncompetitive
2,3-Dimercaptopropanol
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competitive inhibitor to glycerophosphate
2,4-Dichlorophenoxyacetic acid
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-
2-amino-2-hydroxymethylpropane-1,3-diol
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i.e. Tris
2-hydroxy-1,2,3-nonadecanetricarboxylic acid
3-morpholinosydnonimine
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-
adenosine diphosphate ribose
ADP
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at physiological concentration, 10 mM 90% inhibition
ADP-ribose
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allosteric inhibitor
Cd2+
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50% inhibition at 8.33 mM; 50% inhibition at 8.3 mM
Cu2+
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50% inhibition at 12.96 mM; 50% inhibition at 13.0 mM
dihydroxyacetone phosphate
FeCl2
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0.5 mM, about 10% residual activity
fructose-1,6-bisphosphate
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at physiological concentration, non-competitive
glycerol
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slight inhibition
glycerol phosphate
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0.025 mM, strong inhibition of chloroplastic and cytosolic form, endproduct inhibition
guanidine hydrochloride
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-
guanidinium hydrochloride
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gymnemic acid
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may have some pharmacological activities including antidiabetic activity and lipid lowering effects via interaction with G3PDH
iodoacetamide
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effective inhibitor
K+
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50% inhibition at 40.66 mM; 50% inhibition at 40.7 mM
Large peptide factor
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chloroplast enzyme
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linoleic acid
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0.003 mM, 40% inhibition of chloroplastic form and 43% inhibition of cytosolic form
malate
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at high concentration
Mn2+
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50% inhibition at 36.6 mM
NADH-X
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allosteric inhibitor
Ni2+
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50% inhibition at 31.66 mM; 50% inhibition at 31.7 mM
Nucleic acids
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strongly inhibit
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o-Iodosobenzoic acid
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0.5 mM, about 10% residual activity
octyl glucose
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0.003 mM, 41% inhibition of chloroplastic form and 61% inhibition of cytosolic form
p-mercuribenzoate
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0.1 mM complete inhibition
palmitic acid
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0.003 mM, 40% inhibition of chloroplastic form and 43% inhibition of cytosolic form
phenylmethyl sulfonyl fluoride
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0.5 mM 50% inhibition of cytosolic form, little effect on chloroplastic form
phosphatidyl choline
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0.003 mM, 42% inhibition of chloroplastic form and 43% inhibition of cytosolic form
phosphite dianion
strongly inhibits the mutant N270A enzyme. The N270A mutation results in a change in the effect of phosphite dianion on (kcat/Km)obs for GPDH-catalyzed reduction of glycerone phosphate, from strongly activating to inhibiting
phosphogluconate
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cytosolic isozyme
pomolic acid
pomolic acid treatment, after cell differentiation, suppresses the increase in GPDH activity in 3T3-L1 adipocytes and the increase in lipid amounts
reduced thioredoxin
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stimulation of chloroplastic form
S-nitroso-N-acetylpenicillamine
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-
sedoheptulose 1,7-bisphosphate
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0.5 mM, chloroplastic and cytosolic form inhibited by 50%
selenocysteine
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0.015 mM, 10% residual activity
selenomethionine
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0.015 mM, 40% residual activity
Small peptide factor
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cytosolic enzyme
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SO42-
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at high concentration, MgSO4 most inhibitory
Sodium selenite
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0.015 mM, 10% residual activity
Thylakoid fraction
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0.02 mM 97% inhibition
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Triton X-100
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0.006 mM, 50% inhibition of chloroplastic form and 52% inhibition of cytosolic form
Zn2+
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50% inhibition at 5.66 mM; 50% inhibition at 5.7 mM
ZnCl2
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0.5 mM, about 10% residual activity
(NH4)2SO4
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-
(NH4)2SO4
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inhibition of chloroplastic and cytosolic form
2-hydroxy-1,2,3-nonadecanetricarboxylic acid
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trypanocidal drug, IC50 0.00055 mM
2-hydroxy-1,2,3-nonadecanetricarboxylic acid
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IC50 0.0011 mM
adenosine diphosphate ribose
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0.094 mM slightly inhibits NADH binding by honeybee GPDH, but not by rabbit GPDH
adenosine diphosphate ribose
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-
ATP
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weak inhibitor of both isozymes, i.e. GPDH-1 and -3
ATP
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at physiological concentration, 10 mM 95% inhibition
Cl-
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competitive inhibitor with respect to dihydroxyacetone phosphate
Cl-
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cations, i.e. H+, K+, Na+ associated with Cl- do not affect the reduction of dihydroxyacetone phosphate
dihydroxyacetone phosphate
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high levels of substrate, i.e. dihydroxyacetone phosphate result in inhibition
dihydroxyacetone phosphate
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substrate inhibition above 1 mM, NADH above 0.2 mM; substrate inhibition only at high concentration, over 1 mM
dihydroxyacetone phosphate
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0.5 mM, GPDHs more susceptible to inhibition
dihydroxyacetone phosphate
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substrate inhibition at 0.2 mM
dihydroxyacetone phosphate
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substrate inhibition at 0.2 mM
iodoacetate
-
-
iodoacetate
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50 mM, incubated for 60 min
iodoacetate
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0.1 mM 23% inhibition
iodoacetate
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reversible by dithiothreitol, 10 mM inhibits to 50%
L-glycerol 3-phosphate
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inhibits dihydroxyacetone phosphate reduction
L-glycerol 3-phosphate
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-
L-glycerol 3-phosphate
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inhibitor of bumble bee enzyme, non-competitive
L-glycerol 3-phosphate
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competitive inhibitor to dihydroxyacetone phosphate, non-competitive to NADH
L-glycerol 3-phosphate
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inhibits dihydroxyacetone phosphate reduction
L-glycerol 3-phosphate
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over 0.025 mM, strong inhibitor of cytosolic and chloroplastic enzyme
Melarsen oxide
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active principle of the trypanocidal drug melarsoprol and cymelarsen
Melarsen oxide
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active principle of the trypanocidal drug melarsoprol and cymelarsen; cymelarsen, IC50 0.0015-0.005 mM
N-ethylmaleimide
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0.1 mM inhibits enzyme over 60%
N-ethylmaleimide
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1 mM results in 50% inhibition, reversible by NADH, inhibition increases in the presence of dihydroxyacetone phosphate and/or glycerol 3-phosphate
N-ethylmaleimide
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0.5 mM, about 20% residual activity
N-ethylmaleimide
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20 mM, complete inhibition; 20 mM, complete loss of activity
N-ethylmaleimide
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0.1 mM complete inhibition
N-ethylmaleimide
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reversible by dithiothreitol, 5 mM inhibits more than 90% of the enzyme activity
NaCl
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inactivation
NaCl
isozyme GPDH1 is severely inhibited by the addition of 100-200 mM NaCl; isozyme GPDH2 is severely inhibited by the addition of 100-200 mM NaCl
NaCl
-
strongly inhibits, 50% activity at 250 mM NaCl
NaCl
-
inactivates irreversibly
NaCl
-
strongly inhibits, 50% activity at 250 mM NaCl
NAD+
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competitive inhibitor to NADH at physiological concentration; non-competitive to dihydroxyacetone phosphate
NAD+
-
competitive inhibitor to NADH at physiological concentration
NAD+
-
competitive inhibitor to NADH at physiological concentration
NADH
-
at high concentration
NADH
-
at high concentration
NADPH
-
-
NADPH
-
inhibits in presence of saturing concentration of NADH and dihydroxyacetone phosphate
NADPH
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inhibits in presence of saturing concentration of NADH and dihydroxyacetone phosphate
p-chloromercuribenzoate
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0.0001 mM inhibits enzyme over 60%
p-chloromercuribenzoate
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0.05 mM, 100% inhibition
p-chloromercuribenzoate
-
effective inhibitor
p-chloromercuribenzoate
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10 nM, strong inhibition
p-chloromercuribenzoate
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10 nM, strong inhibition; reversible by dithiothreitol, 0.001 mM inhibits more than 90% of the enzyme activity
p-chloromercuribenzoate
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0.1 mM, reversed by thiols, e.g. dithiothreitol
phosphate
-
competitive inhibition
phosphate
phosphate at 5-10 mM severely inhibits the enzymatic activity of isozyme GPDH1; phosphate at 5-10 mM severely inhibits the enzymatic activity of isozyme GPDH2
phosphate
-
competitive inhibitor against dihydroxyacetone phosphate, non-competitive inhibitor against NADH
phosphate
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slight inhibition of cytosolic form, at higher concentrations above 20-30 mM both forms are inhibited
suramin
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trypanocidal drug, potent inhibitor, IC50 0.0002 mM
suramin
-
IC50 0.00044 mM
additional information
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high ionic strength above 0.03 M
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additional information
GPDH1 transcript level decreases progressively with NaCl concentrations above 3-5 M, the expression level of GPDH1 in 5 M NaCl is only approximately a quarter of that in 2 M NaCl; the GPDH2 transcript level decreases to less than half the level in 1 M NaCl
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additional information
GPDH1 transcript level decreases progressively with NaCl concentrations above 3-5 M, the expression level of GPDH1 in 5 M NaCl is only approximately a quarter of that in 2 M NaCl; the GPDH2 transcript level decreases to less than half the level in 1 M NaCl
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additional information
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not inhibitory: CaCl2, MgCl2, NaCl
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additional information
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treatment with 0.075 mg/ml Ascophyllum nodosum extract depressed cellular GPDH activity by approximately 20%
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additional information
oleanolic and ursolic acids have no apparent effect on in 3T3-L1 cells
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additional information
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coenzyme analogs: acetylpyridine-NAD+, deaminoacetylpyridine-NAD+, pyridinealdehyde-NAD+, deaminopyridinealdehyde-NAD+, potent inhibitors
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additional information
no inhibition of the cytosolic NAD+-linked cGPDH enzyme by cell-permeant small-molecule inhibitors of mitochondrial mGPDH, EC 1.1.5.3, with a core benzimidazole-phenyl-succinamide structure
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additional information
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the hyperthyroid status leads to a significant decrease of both enzyme amount and activity in both female and male animals
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additional information
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no inhibition by NADPH, acetaldehyde, glycerol, ethanol
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additional information
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additional information
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cyclic-AMP
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