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1.2.1.104: pyruvate dehydrogenase system

This is an abbreviated version!
For detailed information about pyruvate dehydrogenase system, go to the full flat file.

Reaction

pyruvate
+
CoA
 +
NAD+
=
acetyl-CoA
 +
CO2
 +
NADH

Synonyms

aceE, AceF, At1g54220, At3g13930, At3g52200, CTHT_0006350, CTHT_0069820, dihydrolipoamide acetyltransferase, dihydrolipoyllysine-residue acetyltransferase component, DLAT, DLD, DLST, E1 component of pyruvate dehydrogenase complex, E1 component subunit alpha, E1 component subunit beta, IAR4, LpdA, Lta3, MAB1, More, Mrp-3, Pda1, Pda1p, PDC, PDCp, PDH, PDH complex, PDH-E1 catalytic subunit, PDHa, PdhA1, PDHalpha, PdhB1, PDHC, PdhE, PDHE1alpha1, PdhH, PdhX, PH2, plastidial pyruvate dehydrogenase complex, pyruvate decarboxylase, pyruvate dehydrogenase, pyruvate dehydrogenase alpha subunit, pyruvate dehydrogenase complex, pyruvate dehydrogenase E1

ECTree

     1 Oxidoreductases
         1.2 Acting on the aldehyde or oxo group of donors
             1.2.1 With NAD+ or NADP+ as acceptor
                1.2.1.104 pyruvate dehydrogenase system

Inhibitors

Inhibitors on EC 1.2.1.104 - pyruvate dehydrogenase system

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-(4-bromophenyl)ethanone O-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl)oxime
thiamine diphosphate analog, at 0.1 mM 33% inhibition against Gibberlla zeae
1-(4-chlorophenyl)ethanone O-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl)oxime
thiamine diphosphate analog, at 0.1 mM 35% inhibition against Gibberlla zeae
1-(4-nitrophenyl)ethanone O-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl)oxime
thiamine diphosphate analog, at 0.1 mM 50% inhibition against Gibberlla zeae
1-[3-[4-(1,3,2-dithiarsinan-2-yl)anilino]-3-oxopropyl]-4-[(E)-2-(1H-indol-3-yl)ethenyl]pyridin-1-ium
i.e. PDT-PAO-16, organic arsenal inhibitor, mainly accumulates in mitochondria within hours and suppresses the activity of the pyruvate dehydrogenase complex resulting in the inhibition of ATP synthesis and thermogenesis disorder. The suppression of respiratory chain complex I and IV accelerates the mitochondrial dysfunction leading to caspase family-dependent apoptosis. In vivo, the acute promyelocytic leukemia is greatly alleviated in the PDT-PAO-F16 treated group in an acute promyelocytic leukemia mice model
2,3-Butanedione
Pigeon
-
10 mM, biphasic kinetic, complete inactivation after 20 min
2-([1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-5-iodo-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl)-1H-isoindole-1,3(2H)-dione
potent algaecidal activity against Synechocystis sp. PCC 6803
2-p-Toluidinonaphthalene-6-sulfonate
-
-
3-([1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl)-5-chloroquinazolin-4(3H)-one
-
3-([1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl)-6-bromoquinazolin-4(3H)-one
-
3-([1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-5-iodo-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl)-6-bromoquinazolin-4(3H)-one
potent algaecidal activity against Synechocystis sp. PCC 6803
3-([1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-5-iodo-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl)-6-chloro-1,2,3-benzotriazin-4(3H)-one
-
3-Bromopyruvate
-
-
3-deazathiamine diphosphate
4-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methoxy)benzonitrile
-
exhibits very good enzyme-selective inhibition of PDH-E1 between pig heart and Escherichia coli and activity against Rhizoctonia solani and Botrytis cinerea even at 12.5 lg/ml
4-aminophenyl arsenoxide
0.1 mM, 92% loss of activity in presence of pyruvate and CoA. Controls lacking pyruvate and/or coenzyme A, but containing H2NPhAsO, retain nearly all their pyruvate dehydrogenase complex activity. The arsenoxide forms a stable cyclic dithiolarsinite with reduced lipoic acid on E2 which is generated by pyruvate and coenzyme A according. Pyruvate dehydrogenase complex activity can be recovered to 78% within 2 min following the addition of 2,3-dithiopropanol
5,5'-dithiobis(2-nitrobenzoate)
Pigeon
-
-
5-((4-((4-bromophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
-
exhibits activity against Rhizoctonia solani and Botrytis cinerea even at 12.5 lg/ml
5-((4-((4-chloro-3-methylphenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
-
-
5-((4-((4-chlorophenoxy)methyl)-5-iodo-1H-1,2,3-triazol-1-yl)methyl)-2-methylpyrimidin-4-amine
-
exhibits activity against Rhizoctonia solani even at 12.5 lg/ml and almost 5.5 times more inhibitory potency against Botryttis cinerea than pyrimethanil
acetaldehyde
-
weak
acetyl-CoA
acetylmethylphosphinate
Acetylphosphinate
alpha-Ketobutyric acid
-
-
alpha-Ketocaproate
-
-
alpha-ketooctanoic acid
-
-
alpha-ketovalerate
-
-
beta-Hydroxypyruvate
bromoacetylaniline arsenoxide
BrCH2CONHPhAsO, 0.1 mM, 100% loss of activity in presence of pyruvate and CoA. The initial reaction of the bifunctional reagent occurs on E2 via the R-AsO moiety and results in the rapid loss in pyruvate dehydrogenase complex activity. Addition of 2,3-dithiopropanol fails to regenerate the complex activity and E3 activity
citrate
-
0.25 mM, 29% inhibition, 50.0 mM, 87% inhibition
CoA
allosteric inhibition
CuSO4
EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
diethyldicarbonate
Pigeon
-
-
Fluoropyruvate
gibberellin
-
modulates the activity of enzyme by regulating the expression of pyruvate dehydrogenase kinase1 and subsequently controlling plant growth and development
glyoxylate
glyoxylic acid
-
weak
GTP
-
5 mM, about 50% inhibition after 3 h
Guanidinium chloride
-
treatment of the E2-X subcomplex with 4 M guanidinium chloride causes a complete loss of enzymatic activity and the dissociation of the subcomplex into monomeric 1.5-3 S species. Removal of the chaotrope by dialysis for 18 h results in complete restoration of E2 enzymatic activity and reassembly of a 32 S subcomplex. The reassembled E2-X subcomplex demonstrates the presence of an 8 S assembly intermediate. The 8 S species associates non-cooperatively to yield additional assembly intermediates exhibiting sedimentation coefficients of 10-32 S
illumination
-
mitochondrial pyruvate dehydrogenase complex
-
L-lactate
-
weak
MgATP2-
Moniliformin
-
0.3 mM, 82% inhibition
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl) methyl)-2,4,6-trimethylbenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0043 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl) methyl)-2-nitrobenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0063 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl) methyl)-4-bromobenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.009 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl) methyl)-4-chlorobenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0018 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-2,4,6-trimethylbenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-bromobenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-fluorobenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0017 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-methoxybenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0027 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-methylbenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
-
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-5-iodo-1H-1,2,3-triazol-4-yl)methyl)-4-nitrobenzenesulfonamide
thiamin diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0016 mM, EC50 value against Microcystis aeruginosa FACHB905 is 0.0001 mM
-
N-(3-[(2E)-2-[(4-amino-2-methylpyrimidin-5-yl)methylidene]hydrazinecarbonyl]phenyl)-2-fluorobenzamide
72-92% inhibition against Xanthomonas oryzae pv. Oryzae and Ralstonia solanacearum at 100 microg/ml
N-(3-[(2E)-2-[(4-amino-2-methylpyrimidin-5-yl)methylidene]hydrazinecarbonyl]phenyl)-4-bromobenzamide
negligible inhibition against porcine pyruzvate dehydrogenase complex, 72-92% inhibition against Xanthomonas oryzae pv. Oryzae and Ralstonia solanacearum at 100 microg/ml
N-(3-[(2E)-2-[(4-amino-2-methylpyrimidin-5-yl)methylidene]hydrazinecarbonyl]phenyl)-4-fluorobenzamide
72-92% inhibition against Xanthomonas oryzae pv. Oryzae and Ralstonia solanacearum at 100 microg/ml
N-(3-[(2E)-2-[(4-amino-2-methylpyrimidin-5-yl)methylidene]hydrazinecarbonyl]phenyl)-4-methylbenzamide
negligible inhibition against porcine pyruzvate dehydrogenase complex
N-(3-[(2E)-2-[(4-amino-2-methylpyrimidin-5-yl)methylidene]hydrazinecarbonyl]phenyl)butanamide
72-92% inhibition against Xanthomonas oryzae pv. Oryzae and Ralstonia solanacearum at 100 microg/ml
N-(4-[(2E)-2-[(4-amino-2-methylpyrimidin-5-yl)methylidene]hydrazinecarbonyl]phenyl)-4-bromobenzamide
negligible inhibition against porcine pyruzvate dehydrogenase complex
N-(4-[(2E)-2-[(4-amino-2-methylpyrimidin-5-yl)methylidene]hydrazinecarbonyl]phenyl)-N'-phenylurea
negligible inhibition against porcine pyruzvate dehydrogenase complex, 72-92% inhibition against Xanthomonas oryzae pv. Oryzae and Ralstonia solanacearum at 100 microg/ml
Oxythiamine diphosphate
p-chloromercuribenzoate
Pigeon
-
0.026 mM, complete inactivation after 80 s
PDC kinase II
-
phosphorylates and inactivates Pda1p
-
Phenylglyoxal
Pigeon
-
10 mM, biphasic kinetic, complete inactivation after 30 min
phenylpyruvate
-
-
phosphorylation
-
protein Pkp1p
-
phosphorylates and inactivates Pda1p
-
Pyruvamide
-
acts as substrate analogue, competitive
pyruvate dehydrogenase kinase
-
deactivates PDH by phosphorylation
-
Sodium diphosphate
-
competitive vs. thiamine diphosphate
tellurite
-
pyruvate dehydrogenase activity decreases by 81% after tellurite treatment (0.0005 mg/ml for 30 min)
thiamin 2-thiazolone diphosphate
tight-binding inhibitor, binds via a two-step mechanism,
thiamin 2-thiothiazolone diphosphate
tight-binding inhibitor, binds via a two-step mechanism to wild-type, but to mutant Y177A via a one-step mechanism
thiamine 2-thiothiazolone diphosphate
-
-
tryptamine-4,5-dione
-
inhibition is blocked by reduced glutathione or cysteine at large molar excess, ascorbate protects partially
[1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-5-iodo-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl 3-chlorobenzoate
-
[1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-5-iodo-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl 4-chlorobenzoate
compound shows inhibitory selectivity between Synechocystis sp. pyruvate dehydrogenase complex E1 (inhibitory rate 98.90%) and porcine pyruvate dehydrogenase complex E1 (inhibitory rate 9.54%)
[1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-5-iodo-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl 4-fluorobenzoate
-
[1-[(4-amino-2-methylpyrimidin-5-yl)methyl]-5-iodo-4,5-dihydro-1H-1,2,3-triazol-4-yl]methyl 4-nitrobenzoate
-
additional information
-