2.1.1.148: thymidylate synthase (FAD)
This is an abbreviated version!
For detailed information about thymidylate synthase (FAD), go to the full flat file.
Word Map on EC 2.1.1.148
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2.1.1.148
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medicine
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tuberculosis
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dtmp
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synthases
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thymidine
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dihydrofolate
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maritima
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bursaria
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2'-deoxyuridine
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paramecium
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folate-dependent
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chlorella
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5-substituted
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virus-1
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ch2h4folate
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2'-deoxythymidine-5'-monophosphate
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flavoenzyme
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drug development
- 2.1.1.148
- medicine
- tuberculosis
- dtmp
- synthases
- thymidine
- dihydrofolate
- maritima
- bursaria
- 2'-deoxyuridine
-
paramecium
-
folate-dependent
- chlorella
-
5-substituted
-
virus-1
-
ch2h4folate
-
2'-deoxythymidine-5'-monophosphate
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flavoenzyme
- drug development
Reaction
Synonyms
A674R, complementing thymidylate synthase, FDTS, flavin dependent thymidylate synthase, flavin-dependent thymidylate synthase, flavin-dependent thymidylate synthase X, flavin-dependent TS, Thy1, thymidylate synthase 1, thymidylate synthase complementing protein, thymidylate synthase ThyX, thymidylate synthase X, ThyX, thyX-encoded thymidylate synthase, TSCP, TTHA1096
ECTree
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Inhibitors
Inhibitors on EC 2.1.1.148 - thymidylate synthase (FAD)
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(2R)-2-[(3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazin-6-yl)sulfanyl]propanoic acid
6% inhibition at 0.1 mM
(heptanoyl[[(4R)-2-phenyl-3-(phenylcarbonyl)-1,3-thiazolidin-4-yl]methyl] amino)acetic acid
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2-(furan-2-yl)-3-hydroxynaphthalene-1,4-dione
inhibits the NADPH oxidation and 2'-deoxythymidine-5'-monophosphate-forming activities of ThyX in vitro
2-hydroxy-3-(4-methoxyphenyl)naphthalene-1,4-dione
inhibits the NADPH oxidation and 2'-deoxythymidine-5'-monophosphate-forming activities of ThyX in vitro
2-hydroxy-3-propylnaphthalene-1,4-dione
inhibits the NADPH oxidation and 2'-deoxythymidine-5'-monophosphate-forming activities of ThyX in vitro, significant decrease of 1.22 log (17fold) in the colonization loads with Helicobacter pylori of mice treated with the molecule
2-[4-fluoro-3-(trifluoromethyl)phenyl]-3-hydroxynaphthalene-1,4-dione
inhibits the NADPH oxidation and 2'-deoxythymidine-5'-monophosphate-forming activities of ThyX in vitro
4-(3-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)propanoyl)-N-phenylpiperazine-1-carboxamide
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4-[3-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)propanoyl]-N-phenylpiperazine-1-carboxamide
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8-aminopurinone deoxyribonucleoside 5'-phosphate
Paramecium bursaria Chlorella virus-1
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0.05 mM, 50% inhibition
diethyldicarbonate
Paramecium bursaria Chlorella virus-1
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decreases ThyX deprotonation activity at least 20fold, is partially reversible with hydroxylamine treatment
ethyl (4R)-2-phenyl-3-([(1-(3-2,2,2-trifluoroacetamido)propyl)-1H-1,2,3-triazol-4-yl]carbonyl)-1,3-thiazolidine-4-carboxylate
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ethyl (4R)-2-phenyl-3-[[1-(2-thiophen-3-ylethyl)-1H-1,2,3-triazol-4-yl]carbonyl]-1,3-thiazolidine-4-carboxylate
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ethyl (4R)-3-([1-[2-(4-fluorophenyl)ethyl]-1H-1,2,3-triazol-4-yl]carbonyl)-2-phenyl-1,3-thiazolidine-4-carboxylate
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ethyl (4R)-3-[[1-(7-hydroxyheptyl)-1H-1,2,3-triazol-4-yl]carbonyl]-2-phenyl-1,3-thiazolidine-4-carboxylate
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N-methyl-2-[4-[3-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)propanoyl]piperazin-1-yl]-N-phenylacetamide
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N-[1-[3-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)propanoyl]piperidin-4-yl]-N'-phenylurea
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tetrahydrofolate
competitively inhibits the oxidase activity of the enzyme, which indicates that tetrahydrofolate and O2 compete for the same reduced and dUMP-activated enzymatic complex
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no activity against classical thymidylate synthase ThyA, EC 2.1.1.45
5-undecyloxymethyl-2'-deoxyuridine 5'-monophosphate
compound lacks activity against isoform ThyA, EC 2.1.1.45
NADPH
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inhibits FDTS at high concentrations at all temperatures, NADPH may not be the natural reducing agent of FDTS
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functional evidence for active site location of tetrameric thymidylate synthase X at the interphase of three monomers. The active-site configurations of ThyX proteins, present in many human pathogenic bacteria, and of human thymidylate synthase A (EC 2.1.1.45) are different.
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additional information
Paramecium bursaria Chlorella virus-1
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no inhibition by 10-propargyl-5,6-dideazafolate, 10-methylfolate, 8-azapurinone deoxyribonucleoside 5-phosphate
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additional information
Paramecium bursaria Chlorella virus-1
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5-fluorouracil is not a potential inhibitor
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