2.1.1.45: thymidylate synthase
This is an abbreviated version!
For detailed information about thymidylate synthase, go to the full flat file.
Word Map on EC 2.1.1.45
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2.1.1.45
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5-fluorouracil
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thymidine
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colorectal
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dihydrofolate
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antifolate
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methotrexate
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dihydropyrimidine
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pyrimidine
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fluoropyrimidine
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phosphorylase
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ribonucleotide
-
leucovorin
-
pemetrexed
-
resect
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fdump
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uracil
-
mthfr
-
casey
-
schedule
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polyglutamates
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non-small
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cisplatin
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folylpolyglutamate
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deoxyuridine
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oxaliplatin
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5-fluoro-2'-deoxyuridine
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antimetabolite
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orotate
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irinotecan
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capecitabine
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5-fu-based
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ccrf-cem
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folate-dependent
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gemcitabine
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folinic
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formyltransferase
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quinazoline
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glycinamide
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dttp
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polyglutamylation
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2'-deoxyuridine
-
tegafur
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medicine
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methotrexate-resistant
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deoxycytidylate
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cross-complementing
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drug development
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transformylase
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5-fu-induced
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dutpase
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aminopterin
-
deoxythymidine
- 2.1.1.45
- 5-fluorouracil
- thymidine
- colorectal
- dihydrofolate
- antifolate
- methotrexate
- dihydropyrimidine
- pyrimidine
-
fluoropyrimidine
- phosphorylase
- ribonucleotide
- leucovorin
- pemetrexed
-
resect
- fdump
- uracil
- mthfr
-
casey
-
schedule
- polyglutamates
-
non-small
- cisplatin
- folylpolyglutamate
- deoxyuridine
- oxaliplatin
- 5-fluoro-2'-deoxyuridine
-
antimetabolite
- orotate
- irinotecan
- capecitabine
-
5-fu-based
-
ccrf-cem
-
folate-dependent
- gemcitabine
-
folinic
-
formyltransferase
- quinazoline
- glycinamide
- dttp
-
polyglutamylation
- 2'-deoxyuridine
-
tegafur
- medicine
-
methotrexate-resistant
- deoxycytidylate
-
cross-complementing
- drug development
-
transformylase
-
5-fu-induced
- dutpase
- aminopterin
- deoxythymidine
Reaction
Synonyms
BgDHFR-TS, bifunctional TS-DHFR, DFR-TS, DHFR-TS, DHFR–TS, dihydrofolate reductase-thymidylate synthase, dTMP synthase, HTS, human TS, LBRM_06_0830, methylenetetrahydrofolate:dUMP C-methyltransferase, More, Thy1, ThyA, thymidylate synthase, thymidylate synthase A, thymidylate synthase-dihydrofolate reductase, thymidylate synthetase, ThyX, TMP synthetase, TMPS, TS, TS-DHFR, TSase, TYMS, Y110A7A.4
ECTree
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KI Value
KI Value on EC 2.1.1.45 - thymidylate synthase
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0.000018
(2R)-2-(5-[[(1-hydroxy-3-methyl-5,10a-dihydrobenzo[f]quinazolin-9-yl)methyl]amino]-1-oxo-1,3-dihydro-2H-isoindol-2-yl)butanedioic acid
22°C
0.12
1-(beta-D-2'-deoxyribofuranosyl)-1,6-dihydro-8-azapurin-2(3H,6H)-one 5'-monophosphate
-
-
0.022 - 0.0321
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate
0.0049 - 0.0085
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate
0.0008 - 0.0014
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate
0.0013 - 0.00191
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate
0.0034 - 0.00746
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate
0.0017 - 0.0093
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate
0.002
2-(4-hydroxy[1,1'-biphenyl]-3-yl)-4-methyl-1H-isoindole-1,3(2H)-dione
pH not specified in the publication, temperature not specified in the publication
0.013
2-[2-(3-methoxyphenoxy)propyl]-4-methyl-1H-isoindole-1,3(2H)-dione
pH not specified in the publication, temperature not specified in the publication
0.025
4'-[(4-methyl-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl][1,1'-biphenyl]-2-carbonitrile
pH not specified in the publication, temperature not specified in the publication
0.024
4,5,6,7-tetrachloro-2-[3-(phenylsulfanyl)propyl]-1H-isoindole-1,3(2H)-dione
pH not specified in the publication, temperature not specified in the publication
0.022
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L1210 recombinant enzyme
0.0321
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0049
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L1210 recombinant enzyme
0.0085
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0008
-
L1210 parental enzyme
0.0014
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate
-
L1210 recombinant enzyme
0.0013
-
L1210 recombinant enzyme
0.00191
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0034
-
L1210 recombinant enzyme
0.00746
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0017
-
L1210 parental enzyme
0.0093
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 recombinant enzyme
0.000002
5-fluoro-2'-deoxyuridine 5'-monophosphate
inhibited both ThyA and ThyX
0.0011
-
wild type enzyme, in 50 mM TES buffer, 50 mM, MgCl2, 13 mM formalin, 2 mM EDTA, 0.15 mM 2-mercaptoethanol, pH 7.4, at 25°C
0.0054
5-fluoro-2'-deoxyuridine-5'-monophosphate
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mutant enzyme E30W, in 50 mM TES buffer, 50 mM, MgCl2, 13 mM formalin, 2 mM EDTA, 0.15 mM 2-mercaptoethanol, pH 7.4, at 25°C
0.0014
-
1.0 mM, noncompetitive inhibition, 5,10-methylenetetrahydrofolate as variable substrate
0.00178
dihydrofolate
-
5.0 mM, noncompetitive inhibition, 5,10-methylenetetrahydrofolate as variable substrate
0.00294
dihydrofolate
-
0.5 mM, noncompetitive inhibition, dUMP as variable substrate
0.00303
dihydrofolate
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1.0 mM, noncompetitive inhibition, dUMP as variable substrate
0.00022
Procion blue
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variable substrate 5,10-methylenetetrahydropteroylglutamate
0.0000059
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wild type enzyme, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C
0.0000113
propylene diphosphonate
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mutant enzyme A191K, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C
0.001
-
0.25 mM, noncompetitive inhibition, 5,10-mehylenetetrahydrofolate as variable substrate
0.00124
thymidine phosphate
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1.0 mM, noncompetitive inhibition, 5,10-methylenetetrahydrofolate as variable substrate
0.3125
thymidine phosphate
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0.25 mM, competitive inhibition, dUMP as variable substrate
additional information
DHFR inhibition kinetics
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additional information
additional information
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DHFR inhibition kinetics
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