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1.2.4.1: pyruvate dehydrogenase (acetyl-transferring)

This is an abbreviated version!
For detailed information about pyruvate dehydrogenase (acetyl-transferring), go to the full flat file.

Word Map on EC 1.2.4.1

Reaction

pyruvate
+
[dihydrolipoyllysine-residue acetyltransferase] lipoyllysine
=
[dihydrolipoyllysine-residue acetyltransferase] S-acetyldihydrolipoyllysine
+
CO2

Synonyms

aceE, AcoA, CTHT_0006350, CTHT_0069820, dehydrogenase, pyruvate, E1 component of pyruvate dehydrogenase, E1 component of pyruvate dehydrogenase multienzyme complex, E1 component of the pyruvate dehydrogenase multienzyme complex, E1 component subunit alpha, E1 component subunit beta, E1alpha, E1ec, E1p, IAR4, MAB1, MdeB, mitochondrial pyruvate dehydrogenase, More, MtPDC, OsI_14647, OsI_31986, Pda1, PDC, PDH, PDH E1alpha, PDH subunit E1-beta, PDH-A1, PDHa, PdhA1, PDHA1a, PdhB, PDHC, PDHc E1, PDHc-E1, PdhE, PDHE1alpha, PdhH, PH2, pyruvate decarboxylase, pyruvate dehydrogenase, pyruvate dehydrogenase complex, pyruvate dehydrogenase complex E1 component, pyruvate dehydrogenase complex,, pyruvate dehydrogenase E1, pyruvate dehydrogenase E1 alpha subunit, pyruvate dehydrogenase E1 component, pyruvate dehydrogenase E1 component subunit beta, pyruvate dehydrogenase multienzyme complex, pyruvate dehydrogenase multienzyme complex E1, pyruvate dehydrogenase, E1, pyruvate:NAD oxidoreductase, pyruvate:[dihydrolipoyllysine-residue acetyltransferase]-lipoyllysine 2-oxidoreductase (decarboxylating, acceptor-acetylating), pyruvic acid dehydrogenase, pyruvic dehydrogenase, thiamin diphosphate-dependent pyruvate dehydrogenase, thiamin-dependent pyruvate dehydrogenase, thiamine diphosphate-dependent 2-oxo acid decarboxylase, VEG220, Vegetative protein 220

ECTree

     1 Oxidoreductases
         1.2 Acting on the aldehyde or oxo group of donors
             1.2.4 With a disulfide as acceptor
                1.2.4.1 pyruvate dehydrogenase (acetyl-transferring)

Inhibitors

Inhibitors on EC 1.2.4.1 - pyruvate dehydrogenase (acetyl-transferring)

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2-chlorophenyl)(dimethoxyphosphoryl)methyl [3-(trifluoromethyl)phenoxy]acetate
-
(3,4-dichlorophenyl)(dimethoxyphosphoryl)methyl [3-(trifluoromethyl)phenoxy]acetate
-
(3-chlorophenyl)(dimethoxyphosphoryl)methyl [3-(trifluoromethyl)phenoxy]acetate
-
(4-chlorophenyl)(dimethoxyphosphoryl)methyl [3-(trifluoromethyl)phenoxy]acetate
-
(dimethoxyphosphoryl)(4-methylphenyl)methyl [3-(trifluoromethyl)phenoxy]acetate
-
(dimethoxyphosphoryl)(phenyl)methyl (2,3-dichlorophenoxy)acetate
-
(dimethoxyphosphoryl)(phenyl)methyl (2,6-dichlorophenoxy)acetate
-
(dimethoxyphosphoryl)(phenyl)methyl (2-chloro-5-methylphenoxy)acetate
-
(dimethoxyphosphoryl)(phenyl)methyl (3-fluorophenoxy)acetate
-
(dimethoxyphosphoryl)(phenyl)methyl (4-chloro-2-methylphenoxy)acetate
-
(dimethoxyphosphoryl)(phenyl)methyl (4-chloro-3-methylphenoxy)acetate
-
(dimethoxyphosphoryl)(phenyl)methyl (4-chlorophenoxy)acetate
-
(dimethoxyphosphoryl)(phenyl)methyl (4-fluorophenoxy)acetate
-
1-(dimethoxyphosphoryl)ethyl (2,3-dichlorophenoxy)acetate
-
1-(dimethoxyphosphoryl)ethyl (2,6-dichlorophenoxy)acetate
-
1-(dimethoxyphosphoryl)ethyl (2-chloro-5-methylphenoxy)acetate
-
1-(dimethoxyphosphoryl)ethyl (3-fluorophenoxy)acetate
-
1-(dimethoxyphosphoryl)ethyl (4-chloro-2-methylphenoxy)acetate
-
1-(dimethoxyphosphoryl)ethyl (4-chloro-3-methylphenoxy)acetate
-
1-(dimethoxyphosphoryl)ethyl (4-chlorophenoxy)acetate
-
1-(dimethoxyphosphoryl)ethyl (4-fluorophenoxy)acetate
-
2,2'-Dithiopyridine
-
1.1 mM, 30% inhibition
2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (2,3-dichlorophenoxy)acetate
-
2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (2-chloro-5-methylphenoxy)acetate
-
2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (3-fluorophenoxy)acetate
-
2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (4-chloro-2-methylphenoxy)acetate
-
2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (4-chloro-3-methylphenoxy)acetate
-
2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (4-chlorophenoxy)acetate
-
2,2,2-trichloro-1-(dimethoxyphosphoryl)ethyl (4-fluorophenoxy)acetate
-
3-Bromopyruvate
-
suicide substrate
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
5,5'-dithiobis(2-nitrobenzoate)
-
1.1 mM, 35% inhibition
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
acetyl-CoA
product inhibition, acetyl CoA interacts directly with the E1p component
AgNO3
-
18 mol per mol enzyme, complete inhibition
Aluminium sulfate
-
1.1 mM, 35% inhibition
Ba2+
-
0.11 mM, 10% inhibition
Cd2+
-
0.032 mM, complete inhibition
citrate
-
noncompetitive inhibition
CoA
allosteric inhibition
Cu2+
-
0.36 mM, complete inhibition
CuSO4
EC50 value against Synechocystis sp. PCC 6803 is 0.002 mM
D-glucose
-
treatment of cardiac fibroblasts with 35 mM D-glucose for 72 h reduces the PDH activity remarkably. 0.2 mM thiamine dramatically recovers the high glucose-induced PDH inhibition
EDTA
-
0.036 mM, 40% inhibition, 0.36 mM, complete inhibition, reversed by addition of excess Mg2+ and Ca2+
Fluoropyruvate
-
competitive with respect to pyruvate, both free and complex bound enzyme behave in the same manner
KCl
-
at 2 M, 50% residual activity of enzyme expressed in Escherichia coli
methyl acetylphosphonate
-
phosphonate analogue of pyruvate, leading to formation of a stable 1’,4’-imino-2-alpha-phosphonolactyl-thiamindiphosphate
Methylacetylphosphonate
-
-
MgATP2-
-
due to phosphorylation of the enzyme by pyruvate dehydrogenase kinase
Mn2+
-
0.72 mM
N-((1-((4-amino-2-methylpyrimidin-5-yl)methyl)-1H-1,2,3-triazol-4-yl) methyl)-2,4,6-trimethylbenzenesulfonamide
thiamim 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
thiamim 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
thiamim 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
thiamim 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
thiamim 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
thiamim 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
thiamim 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
thiamim 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
thiamim diphosphate analogue, EC50 value against Synechocystis sp. PCC 6803 is 0.0016 mM, EC50 value against Microcystis aeruginosa FACHB905 is 0.0001 mM
-
N-ethylmaleimide
-
1.1 mM, 50% inhibition
NaBH4
-
rapid inactivation in the presence of thiamine diphosphate, may reduce thiamine diphosphate to produce a reversible inhibitor
NaCl
-
at 2 M, 50% residual activity of enzyme expressed in Escherichia coli
O,O-dimethyl (2,3-dichlorophenoxyacetoxy)(furan-2-yl)-methylphosphonate
-
O,O-dimethyl (2,3-dichlorophenoxyacetoxy)(thien-2-yl)-methylphosphonate
-
O,O-dimethyl (2,4-dichlorophenoxyacetoxy)(furan-2-yl)-methylphosphonate
-
O,O-dimethyl (2,4-dichlorophenoxyacetoxy)(thien-2-yl)-methylphosphonate
-
O,O-dimethyl (2,6-dichlorophenoxyacetoxy)(furan-2-yl)-methylphosphonate
-
O,O-dimethyl (2,6-dichlorophenoxyacetoxy)(thien-2-yl)-methylphosphonate
-
O,O-dimethyl (2-chloro-5-methylphenoxyacetoxy)(furan-2-yl)methylphosphonate
-
O,O-dimethyl (2-chloro-5-methylphenoxyacetoxy)(thien-2-yl)methylphosphonate
-
O,O-dimethyl (3-fluorophenoxyacetoxy)(furan-2-yl)methylphosphonate
-
O,O-dimethyl (3-fluorophenoxyacetoxy)(thien-2-yl)methylphosphonate
-
O,O-dimethyl (4-chloro-2-methylphenoxyacetoxy)(furan-2-yl)methylphosphonate
-
O,O-dimethyl (4-chloro-2-methylphenoxyacetoxy)(thien-2-yl)methylphosphonate
-
O,O-dimethyl (4-chloro-3-methylphenoxyacetoxy)(furan-2-yl)methylphosphonate
-
O,O-dimethyl (4-chloro-3-methylphenoxyacetoxy)(thien-2-yl)methylphosphonate
-
O,O-dimethyl (4-chlorophenoxyacetoxy)(furan-2-yl)methylphosphonate
-
O,O-dimethyl (4-chlorophenoxyacetoxy)(thien-2-yl)methylphosphonate
-
O,O-dimethyl (4-fluorophenoxyacetoxy)(furan-2-yl)methylphosphonate
-
Oxythiamine diphosphate
p-chloromercuribenzenesulfonate
-
8 mol per mol enzyme, complete inhibition
p-chloromercuribenzoate
-
8 mol per mol enzyme, complete inhibition
phosphorylation
-
pyruvate dehydrogenase kinase
-
phosphorylation of E1p by pyruvate dehydrogenase kinase isoforms inactivates the pyruvate dehydrogenase complex
-
sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](2,4-dichlorophenyl)methyl]phosphonate
-
sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](3-nitrophenyl)methyl]phosphonate
-
sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](4-fluorophenyl)methyl]phosphonate
-
sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](4-methoxyphenyl)methyl]phosphonate
-
sodium methyl [[[(2,4-dichlorophenoxy)acetyl]oxy](phenyl)methyl]phosphonate
-
sodium o-methyl (2,4-dichlorophenoxyacetoxy)(2-chlorophenyl)methylphosphonate
-
sodium o-methyl (2,4-dichlorophenoxyacetoxy)(3,4-dichlorophenyl)methyl phosphonate
-
sodium o-methyl (2,4-dichlorophenoxyacetoxy)(4-chlorophenyl)methylphosphonate
-
sodium o-methyl (2,4-dichlorophenoxyacetoxy)(4-methylphenyl)methylphosphonate
-
sodium o-methyl (2,4-dichlorophenoxyacetoxy)(furan-2-yl)methylphosphonate
-
sodium o-methyl (2,4-dichlorophenoxyacetoxy)(pyridin-2-yl)methylphosphonate
-
Tetrahydrothiamine diphosphate
-
cis-isomer, 0.0013 mM, 50% inhibition
thiamine 2-thiazolone diphosphate
crystallization data of complex with enzyme
thiamine 2-thiothiazolone diphosphate
thiamine thiazolone diphosphate
thiamine thiothiazolone diphosphate
-
-
additional information
-