2.2.1.1: transketolase
This is an abbreviated version!
For detailed information about transketolase, go to the full flat file.
Word Map on EC 2.2.1.1
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2.2.1.1
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thiamin
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pentose
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erythrocyte
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pyrophosphate
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transaldolase
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glucose-6-phosphate
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tpp
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ribose
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5-phosphate
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aldolase
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non-oxidative
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glycation
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encephalopathy
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pyridoxine
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apoenzyme
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phosphoglycerate
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wernicke
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baker
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oxythiamine
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neuropathy
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ribose-5-phosphate
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thiamine-deficient
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xylulose
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thiamine-dependent
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6-phosphogluconate
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riboflavin
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calvin
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pharmacology
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drug development
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biotechnology
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pentose-phosphate
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xylulokinase
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industry
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alpha-ketoglutarate
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dihydroxyacetone
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warburg
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phosphoketolase
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3-epimerase
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hemolysates
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pyrophosphokinase
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xylitol
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phosphoribulokinase
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thiaminase
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hydroxypyruvate
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aminopyrimidine
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fructose-6-phosphate
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medicine
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fructose-1,6-bisphosphate
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antivitaminous
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erythrose
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egypt
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thdp-dependent
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diphosphate-dependent
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synthesis
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isotopomer
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analysis
- 2.2.1.1
- thiamin
- pentose
- erythrocyte
- pyrophosphate
- transaldolase
- glucose-6-phosphate
- tpp
- ribose
- 5-phosphate
- aldolase
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non-oxidative
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glycation
- encephalopathy
- pyridoxine
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apoenzyme
- phosphoglycerate
- wernicke
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baker
- oxythiamine
- neuropathy
- ribose-5-phosphate
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thiamine-deficient
- xylulose
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thiamine-dependent
- 6-phosphogluconate
- riboflavin
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calvin
- pharmacology
- drug development
- biotechnology
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pentose-phosphate
- xylulokinase
- industry
- alpha-ketoglutarate
- dihydroxyacetone
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warburg
- phosphoketolase
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3-epimerase
- hemolysates
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pyrophosphokinase
- xylitol
- phosphoribulokinase
- thiaminase
- hydroxypyruvate
- aminopyrimidine
- fructose-6-phosphate
- medicine
- fructose-1,6-bisphosphate
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antivitaminous
- erythrose
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egypt
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thdp-dependent
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diphosphate-dependent
- synthesis
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isotopomer
- analysis
Reaction
Synonyms
glycolaldehydetransferase, STM14_2885, STM14_2886, TK16, TKA, TKL, TKL1, Tkl2, TKT, TKT10, TKT3, TKT7, TktA, TktB, TKTc, TKTL-1, TKTL1, TKTL2, TKTp, transketolase, transketolase 10, transketolase 3, transketolase 7, transketolase A, transketolase B, transketolase like 1, transketolase-1, transketolase-like 1, transketolase-like enzyme 1, transketolase-like-1, transketolase-like-1-gene, transketolase-like-2
ECTree
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Inhibitors
Inhibitors on EC 2.2.1.1 - transketolase
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1-(3-chloro-2-methylphenyl)-3-(2-hydroxy-5-nitrophenyl)urea
inhibitor designed to cover a hot spot in the dimerization interface of the homodimer of the enzyme
1-(5-chloro-2-hydroxy-4-nitrophenyl)-3-phenylurea
inhibitor designed to cover a hot spot in the dimerization interface of the homodimer of the enzyme
1-(5-hydroxynaphthalen-1-yl)-3-(2-methyl-5-nitrophenyl)urea
inhibitor designed to cover a hot spot in the dimerization interface of the homodimer of the enzyme
2-[(2,2-dimethyl-2,3-dihydro-1-benzofuran-7-yl)oxy]-N-[1-(4-ethyl-6-hydroxypyrimidin-2-yl)-4-(furan-2-yl)-1H-pyrrol-2-yl]acetamide
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3-(2,4-dichlorophenoxy)-N-[3-(furan-2-yl)-1-(pyrimidin-2-yl)-1H-pyrazol-5-yl]propanamide
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3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride
D-ribose 5-phosphate
exerts a time-dependent inhibiting action on enzyme activity in the presence of NaCNBH3
deazathiamine
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retains thiamine pyrophosphokinase activity. Despite improvements in binding to transketolase in enzymatic assays, cell potency relative to the thiazolones and charged thiamine mimetics decrease
fructose 6-phosphate
at concentrations higher than 10 mM fructose 6-phosphate causes an inhibition of the enzyme
N-[1-(3-chloro-5-methylpyridin-2-yl)-3-(furan-2-yl)-1H-pyrazol-5-yl]-3-phenoxypropanamide
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N3P-TT
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an aminopyridine, which possesses low micromolar cellular potency against transketolase
oxidized dithiothreitol
in the absence of Mg2+, the enzyme is strongly inhibited by oxidation, retaining 20-30 % of its control activity when exposed to 50 mM oxidized dithiothreitol. The apoenzyme is 80% inactivated following incubation in the presence of identical amount of oxidized dithiothreitol
p-hydroxyphenylpyruvate
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potent inhibitor when hydroxypyruvate is used as a substrate, whereas noncompetitive inhibition with fructose-6-phosphate
phosphate buffer
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20 mM phosphate buffer shows an inhibitory effect of the enzyme activity of approximately 40%
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thiamine thiazolone
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retains thiamine pyrophosphokinase activity, is a significantly better binder to transketolase than thiamine
thiamine thiazolone diphosphate
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is a significantly better binder to transketolase than thiamine
Urea
denaturation of holo-transketolase by urea displays at least three transitions, where only the final equilibrium denaturation transition is the same for both apo-transketolase and holo-transketolase. Enzyme is deactivated initially by changes in structure associated with the cofactors, but this event does not release the cofactor from the enzyme. Holo-transketolase does not denature to apo-transketolase at 2 M urea. Complete dissociation of cofactors from holo-transketolase at 3.8 M urea without formation of the compact form of apo-transketolase (intermediate form). Holo-transketolase and apo-transketolase at 7.2 M urea both show a common denatured form
ZINC12007063
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i.e. 2-[(2,2-dimethyl-3H-benzofuran-7-yl)oxy]-N-[2-(4-ethyl]-6-oxo-1H-pyrimidin-2-yl)-5-(2-furyl)pyrazol-3
3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride
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analog of thiamine, almost completely suppresses transketolase activity in blood, spleen, and tumor cells, but has little effect on activity of the other thiamine-utilizing enzymes alpha-ketoglutarate dehydrogenase or glucose-6-phosphate dehydrogenase
3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride
analog of thiamine, potent transketolase inhibitor but suffers from poor pharmacokinetics due to high clearance and Cmax linked toxicity. Efficient way of improving the pharmacokinetic profile is to prepare oxidized prodrugs which are slowly reduced in vivo yielding longer, sustained blood levels of the drug
oxythiamine
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inhibitory on proliferation of insulinoma cell line INS-1; when IPCs are cultured with oxythiamine, transketolase activity and insulin gene expression are suppressed
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transketolase-like-1 gene is significantly downregulated in human colon cancer cell line cells transfected with small interfering RNA transketolase-like-1 constructs compared with cells transfected with control vector and cells without transfection. Anti-transketolase-like-1 small interfering RNA construct significantly decreases the level of transketolase in the transfected human colon cancer cell line cells, arrests them in G0/G1 phase and substantially inhibits cell proliferation
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RNAi
inhibits expression of TKTL1, whereas total transketolase activity is dramatically downregulated and proliferation of cancer cells is significantly inhibited in CNE cells
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after 3 h incubation with 50 mM oxidized dithiothreitol, the activity of the enzyme bound to thiamine diphosphate and Mg2+ is almost unaffected, retaining more than 90% of the control (reduced) enzyme activity
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additional information
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after 3 h incubation with 50 mM oxidized dithiothreitol, the activity of the enzyme bound to thiamine diphosphate and Mg2+ is almost unaffected, retaining more than 90% of the control (reduced) enzyme activity
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additional information
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Escherichia coli BL21-Gold(DE3) pQR711 has transketolase activity of ca. 6fold lower than JM107 pQR711 and JM109 pQR711
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additional information
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activity of transketolase is significantly reduced in brains of alcoholic patients with Wernicke-Korsakoffs Syndrome. Reduced transketolase protein expression levels in autopsied prefrontal white and grey matter and cerebellar vermis samples from neurologically uncomplicated alcoholics and alcoholics with liver cirrhosis
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additional information
oxythiamine, inhibitor of human enzyme, is not inhibitory up to 0.03 mM. Instead, oxythiamine, at this concentration, increases the rate of the reaction by 30% under the assay conditions tested. 5-benzyl-3-phenylpyrazolo[1,5-a]pyrimidin-7(4H)-one also has no inhibitory effect
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additional information
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oxythiamine, inhibitor of human enzyme, is not inhibitory up to 0.03 mM. Instead, oxythiamine, at this concentration, increases the rate of the reaction by 30% under the assay conditions tested. 5-benzyl-3-phenylpyrazolo[1,5-a]pyrimidin-7(4H)-one also has no inhibitory effect
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