Information on EC 2.1.1.45 - thymidylate synthase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea, dsDNA viruses, no RNA stage, unclassified phages

EC NUMBER
COMMENTARY
2.1.1.45
-
RECOMMENDED NAME
GeneOntology No.
thymidylate synthase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
5,10-methylenetetrahydrofolate + dUMP = dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
5,10-methylenetetrahydrofolate + dUMP = dihydrofolate + dTMP
show the reaction diagram
O2 and methylenetetrahydrofolate compete for the reduced enzyme after dUMP binding. dUMP enhances the rate of the oxidative half reaction and while the oxidase reaction is faster than the reaction with methylenetetrahydrofolate, this cofactor slows down the consumption of NADPH in the presence of O2 in accordance with substrate competition. dUMP, the substrate of the oxidative half reaction does not affect the reductive half reaction. In the absence of the second substrate methylenetetrahydrofolate, dUMP enhances the reaction of molecular oxygen with the reduced enzyme
-
REACTION TYPE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
dehalogenation
-
-
-
-
methylene group transfer
-
-
-
-
reductive methylation
-
-
-
-
reductive methylation
-
-
reductive methylation
-
-
reductive methylation
-, P67044
-
reductive methylation
-
-
reductive methylation
A6M9A2, -
-
PATHWAY
KEGG Link
MetaCyc Link
folate transformations II
-
formylTHF biosynthesis
-
Metabolic pathways
-
One carbon pool by folate
-
pyrimidine deoxyribonucleosides salvage
-
pyrimidine deoxyribonucleotides biosynthesis from CTP
-
pyrimidine deoxyribonucleotides de novo biosynthesis I
-
pyrimidine deoxyribonucleotides de novo biosynthesis II
-
pyrimidine deoxyribonucleotides de novo biosynthesis IV
-
Pyrimidine metabolism
-
superpathway of pyrimidine deoxyribonucleotides de novo biosynthesis (E. coli)
-
SYSTEMATIC NAME
IUBMB Comments
5,10-methylenetetrahydrofolate:dUMP C-methyltransferase
-
SYNONYMS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
BgDHFR-TS
B5U9U8
-
DHFR-TS
B5U9U8
-
DHFR-TS
Q27793
-
dihydrofolate reductase-thymidylate synthase
B5U9U8
-
dihydrofolate reductase-thymidylate synthase
-
bifunctional enzyme
dihydrofolate reductase-thymidylate synthase
-
-
dihydrofolate reductase-thymidylate synthase
Q27793
-
dTMP synthase
-
-
-
-
human TS
-
-
methylenetetrahydrofolate:dUMP C-methyltransferase
-
-
-
-
ThyA
Corynebacterium glutamicum ATCC 13032, Corynebacterium glutamicum NCHU 87078
-
-
-
thymidylate synthase
-
-
thymidylate synthase A
-
-
thymidylate synthase A
-
-
-
thymidylate synthase-dihydrofolate reductase
-
bifunctional enzyme
thymidylate synthetase
-
-
-
-
thymidylate synthetase
-
-
TMP synthetase
-
-
-
-
TMPS
-
-
TS-DHFR
-
-
TSase
-
-
TYMS
-
-
Y110A7A.4
Caenorhabditis elegans Bristol N2
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
9031-61-2
-
ORGANISM
COMMENTARY
LITERATURE
SEQUENCE CODE
SEQUENCE DB
SOURCE
Abies sp.
pine
-
-
Manually annotated by BRENDA team
metastrongyloid nematode, synonym Parastrongylus
-
-
Manually annotated by BRENDA team
bifunctional dihydrofolate reductase-thymidylate synthase
-
-
Manually annotated by BRENDA team
strain Bristol N2
-
-
Manually annotated by BRENDA team
Caenorhabditis elegans Bristol N2
strain Bristol N2
-
-
Manually annotated by BRENDA team
Clostridium difficile
-
-
-
Manually annotated by BRENDA team
Corynebacterium glutamicum NCHU 87078
-
-
-
Manually annotated by BRENDA team
host Anopheles strain ATCC 11,745
-
-
Manually annotated by BRENDA team
-
P45351
SwissProt
Manually annotated by BRENDA team
encapsulated yeast-like fungus, GenBank accession No.
P45351
SwissProt
Manually annotated by BRENDA team
carrot, wild and culture form
-
-
Manually annotated by BRENDA team
synonym Enterococcus faecalis, strain R
-
-
Manually annotated by BRENDA team
synonym Enterococcus faecium
-
-
Manually annotated by BRENDA team
var. durans
-
-
Manually annotated by BRENDA team
strain B; strain EM 20031 K12; strain K12
-
-
Manually annotated by BRENDA team
strain B; strain K12
-
-
Manually annotated by BRENDA team
strain B; strain R2
-
-
Manually annotated by BRENDA team
Escherichia coli EM 20031 K12
strain EM 20031 K12
-
-
Manually annotated by BRENDA team
Escherichia coli K12
strain K12
-
-
Manually annotated by BRENDA team
Escherichia coli R2
strain R2
-
-
Manually annotated by BRENDA team
GVE2, deep-sea thermophilic bacteriophage
-
-
Manually annotated by BRENDA team
; patients with advanced colorectal carcinoma
-
-
Manually annotated by BRENDA team
; patients with advanced non-small cell lung cancer
-
-
Manually annotated by BRENDA team
AML cells; human; MCF-7 breast cancer cells
-
-
Manually annotated by BRENDA team
HeLa cells
-
-
Manually annotated by BRENDA team
HeLa cells; MCF-7 breast cancer cells
-
-
Manually annotated by BRENDA team
human
UniProt
Manually annotated by BRENDA team
human colon tumor cell line HCT116/200-10
-
-
Manually annotated by BRENDA team
human colorectal tumor cell line C
-
-
Manually annotated by BRENDA team
human sarcome HT1080 cells
-
-
Manually annotated by BRENDA team
human; neoplastic leukemic CCRF-CEM cells
-
-
Manually annotated by BRENDA team
MCF-7 breast cancer cells
-
-
Manually annotated by BRENDA team
neoplastic leukemic CCRF-CEM cells
-
-
Manually annotated by BRENDA team
strain TS N229D, TS N229C
-
-
Manually annotated by BRENDA team
thymidylate synthase chemically synthesized based on the amino acid sequence of TS from Lactobacillus casei
-
-
Manually annotated by BRENDA team
var. rhamnosus, ATCC 7469
-
-
Manually annotated by BRENDA team
Lactobacillus casei TS N229D
strain TS N229D, TS N229C
-
-
Manually annotated by BRENDA team
formerly called Leishmania tropica
-
-
Manually annotated by BRENDA team
albino Swiss mice; Ehrlich ascites carcinoma cells
-
-
Manually annotated by BRENDA team
Ehrlich ascites carcinoma cells; L1210 cells
-
-
Manually annotated by BRENDA team
Gardner lymphosarcoma; mouse, sarcoma 180
-
-
Manually annotated by BRENDA team
L5178 murine leukemia cell line
-
-
Manually annotated by BRENDA team
; isoform ThyX
-
-
Manually annotated by BRENDA team
strain MS11
-
-
Manually annotated by BRENDA team
no activity in Aeropyrum pernix
-
-
-
Manually annotated by BRENDA team
no activity in Aquifex aeolicus
-
-
-
Manually annotated by BRENDA team
no activity in Pyrobaculum aerophilum
-
-
-
Manually annotated by BRENDA team
no activity in Pyrococcus abyssi
-
-
-
Manually annotated by BRENDA team
no activity in Pyrococcus furiosus
DSM 3638
-
-
Manually annotated by BRENDA team
no activity in Pyrococcus horikoshii
-
-
-
Manually annotated by BRENDA team
no activity in Sulfolobus solfataricus
-
-
-
Manually annotated by BRENDA team
no activity in Sulfolobus tokodaii
-
-
-
Manually annotated by BRENDA team
no activity in Thermoplasma acidophilum
-
-
-
Manually annotated by BRENDA team
no activity in Thermoplasma volcanium
-
-
-
Manually annotated by BRENDA team
no activity in Thermotoga maritima
-
-
-
Manually annotated by BRENDA team
strain TM4/8.2
Uniprot
Manually annotated by BRENDA team
Plasmodium falciparum TM4/8.2
strain TM4/8.2
Uniprot
Manually annotated by BRENDA team
H35 hepatoma cells
-
-
Manually annotated by BRENDA team
H35 hepatoma cells; rat
-
-
Manually annotated by BRENDA team
strain Wistar
-
-
Manually annotated by BRENDA team
Rattus norvegicus Wistar
strain Wistar
-
-
Manually annotated by BRENDA team
bakers' yeast; haploid strain
-
-
Manually annotated by BRENDA team
unicellular green algae
-
-
Manually annotated by BRENDA team
wild type strain 8325-4 and trimethoprim-sulfamethoxazole-resistant thymidine-dependent small-colony variants 1-8
-
-
Manually annotated by BRENDA team
industrial strain BMK
-
-
Manually annotated by BRENDA team
causes nagana, the equivalent disease of cattle
-
-
Manually annotated by BRENDA team
causes Chagas' disease in man; sonya strain, maintained in ASH/XP mice
-
-
Manually annotated by BRENDA team
natural pathogen of rats
-
-
Manually annotated by BRENDA team
Trypanosoma rhodesiense
causes human sleeping sickness
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
malfunction
-
growth of single-knockout lines of dihydrofolate reductase-thymidylate synthase in vitro are identical to wild type cells, whereas double-knockout lines of dihydrofolate reductase-thymidylate synthase have an absolute requirement for thymidine
metabolism
-
ThyA is the sole catalyst for thymidylate biosynthesis in Corynebacterium glutamicum
metabolism
Corynebacterium glutamicum NCHU 87078
-
ThyA is the sole catalyst for thymidylate biosynthesis in Corynebacterium glutamicum
-
physiological function
-
thymidylate synthase plays an essential role in embryogenesis, embryos with their thymidylate synthase function inhibited show a retarded embryo development and irregular cell sizes
physiological function
-
DHFRTS is essential for parasite survival
physiological function
C6GJB8, -
thymidylate synthase is the only de novo source of dTMP and is essential for DNA replication
physiological function
Q8QTF3, -
thymidylate synthase is the only de novo source of dTMP and is essential for DNA replication
physiological function
-
the enzyme is essential for the de novo synthesis of DNA
physiological function
-
the enzyme is indispensable for DNA replication in actively dividing cells
physiological function
Caenorhabditis elegans Bristol N2
-
thymidylate synthase plays an essential role in embryogenesis, embryos with their thymidylate synthase function inhibited show a retarded embryo development and irregular cell sizes
-
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
7,8-dihydropteroylglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
-
(-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
7,8-dihydropteroylglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
?
(6R)-N5,N10-methylene-5,6,7,8-tetrahydrofolate + 2'-deoxyuridylate
7,8-dihydrofolate + 5-methyl-2'-deoxyuridylate
show the reaction diagram
P04818
-
-
-
r
(6R)-N5,N10-methylene-5,6,7,8-tetrahydrofolate + 2'-deoxyuridylate
7,8-dihydrofolate + 5-methyl-2'-deoxyuridylate
show the reaction diagram
-
-
-
-
r
(6S)-methylenetetrahydropteroylhexaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylhexaglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
r
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
-
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
r
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
-
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
-
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
-
-
(6S)-tetrahydropteroyltriglutamate + 2'-deoxyuridylate
7,8-dihydropteroyltriglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
r
(R)-5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
(R)-5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
-
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
-
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
thymidylate synthase is the third enzyme in the methylene tetrahydrofolate cycle besides dihydrofolate reductase and serine hydroxymethyltransferase, in many organisms, thymidylate synthase is the only de novo source for dTMP required for DNA synthesis
-
-
?
5,10-methylenetetrahydrofolate + 2'-deoxycytidine 5'-monophosphate
dihydrofolate + cytidine phosphate
show the reaction diagram
Lactobacillus casei, Lactobacillus casei TS N229D
-
only mutant TS N229D
-
-
?
5,10-methylenetetrahydrofolate + 2'-fluoro-2'-deoxyuridine 5'-phosphate
7,8-dihydrofolate + ?
show the reaction diagram
Escherichia coli, Escherichia coli EM 20031 K12, Escherichia coli K12
-
-
-
-
?
5,10-methylenetetrahydrofolate + 5'-fluoro-2'-deoxyuridine 5'-phosphate
7,8-dihydrofolate + ?
show the reaction diagram
-
some mutants are capable of forming covalent thymidylate synthase-5-fluoro-dUMP-methylenetetrahydrofolate complex
-
-
?
5,10-methylenetetrahydrofolate + 6-fluoro-dUMP
?
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + deoxyuridine monophosphate
7,8-dihydrofolate + deoxythymidine monophosphate
show the reaction diagram
B5U9U8, -
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P0CI79
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P0CI79
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P0A884
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P0A884
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P04818
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-, P67044
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P13922
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P13100
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Abies sp.
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P45351
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P45351
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Trypanosoma rhodesiense
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P04818
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Q8QTF3, -
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
C6GJB8, -
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Q27793
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
reverse reaction is at least 630times slower than the forward reaction
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P04818
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P13100
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P45351
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Lactobacillus casei TS N229D
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli EM 20031 K12
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli EM 20031 K12
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Corynebacterium glutamicum NCHU 87078
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Caenorhabditis elegans Bristol N2
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli R2
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli R2
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
tetrahydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
tetrahydrofolate + dTMP
show the reaction diagram
-
-
-
-
-
5,10-methylenetetrahydrofolate + dUMP
tetrahydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
P04818
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-, P67044
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
A6M9A2, -
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
inhibition of thymidylate synthase or of DHFR leads to thymineless death of eukaryotic organisms
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
it is a key enzyme for the synthesis of the DNA-specific nucleotide thymidylate
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
thymidylate synthase catalyses the only de novo pathway to produce thymidylate for DNA replication and repair
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
thymidylate synthase is a key enzyme in the de novo synthesis of dTMP
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
thymidylate synthase is an essential enzyme for de novo synthesis of thymidylate (dTMP), a precursor for DNA synthesis
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
A6M9A2, -
thymidylate synthase is essential for de novo synthesis of dTMP and is a key enzyme involved in DNA synthesis and transcriptional regulation of organisms
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
TS is a key enzyme in folate metabolism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
mTHF, TS is the sole source of de novo thymidylate which is required for DNA synthesis
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + TMP
show the reaction diagram
-
-, during TS inhibition, TMP levels decrease with a subsequent increase in dUTP
-
-
?
5,10-methylenetetrahydrofolate + uridine 5'-phosphate
dihydrofolate + TMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolate + uridine 5'-phosphate
dihydrofolate + TMP
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolylheptaglutamate + 2'-deoxyuridylate
7,8-dihydrofolylheptaglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydrofolylpentaglutamate + 2'-deoxyuridylate
7,8-dihydrofolylpentaglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydropteroylheptaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylheptaglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydropteroylpentaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylpentaglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
r
5,10-methylenetetrahydropteroylpentaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylpentaglutamate + thymidine phosphate
show the reaction diagram
-
-
-
-
r
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
show the reaction diagram
-
dehalogenation
-
-
?
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
show the reaction diagram
-
dehalogenation
-
-
?
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
show the reaction diagram
-
dehalogenation
-
-
?
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
show the reaction diagram
-
dehalogenation does not require methylenetetrahydrofolate as cosubstrate
-
-
?
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
show the reaction diagram
-
dehalogenated by recombinant rat hepatoma enzyme
-
-
?
5-iodo-2'-deoxyuridine 5'-monophosphate + ?
?
show the reaction diagram
-
-
-
-
?
5-iodo-2'-deoxyuridine 5'-monophosphate + ?
?
show the reaction diagram
-
dehalogenation
-
-
?
N5,10-methylenetetrahydrofolate + 2'-deoxyuridine 5'-dithiophosphate
7,8-dihydrofolate + ?
show the reaction diagram
-
-
-
-
?
N5,10-methylenetetrahydrofolate + 2'-deoxyuridine 5'-thiophosphate
7,8-dihydrofolate + ?
show the reaction diagram
-
-
-
-
?
N5,10-methylenetetrahydrofolate + 5-hydroxy-2'-deoxyuridine 5'-monophosphate
7,8-dihydrofolate + ?
show the reaction diagram
-
-
-
-
?
N5,N10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + TMP
show the reaction diagram
-
-, during thymidylate synthase inhibition, TMP levels decrease with a subsequent increase in dUTP
-
-
?
[6R,S]-5,10-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
?
show the reaction diagram
-
-
-
-
-
[6R,S]-5,10-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
?
show the reaction diagram
-
-
-
-
r
[6R]-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
?
show the reaction diagram
-
-
-
-
r
5-iodo-2'-deoxyuridine 5'-monophosphate + ?
?
show the reaction diagram
-
dehalogenated by recombinant rat hepatoma enzyme
-
-
?
additional information
?
-
-
-
-
-
-
additional information
?
-
-
-
-
-
-
additional information
?
-
-
-
-
-
-
additional information
?
-
-
-
-
-
-
additional information
?
-
-
-
-
-
-
additional information
?
-
-
uridylate, cytidylate and deoxycytidylate are not substrates
-
-
-
additional information
?
-
-
dCMP is no substrate, exception mutant TS N229D
-
-
-
additional information
?
-
-
UMP, dCMP and deoxyuridine are no substrates
-
-
-
additional information
?
-
-
inhibitors targeted at human TS designed from structures of bacterial TS may not be optimal
-
-
-
additional information
?
-
-
monofunctional enzyme
-
-
-
additional information
?
-
-
(+) forms are inhibitors
-
-
-
additional information
?
-
-
bifunctional enzyme thymidilate synthase-dihydrofolate reductase, not possible to separate the 2 activities
-
-
-
additional information
?
-
-
nucleotides with large substituents on the 2' position are no substrates, enzyme catalyzes the exchange of a hydrogen atom between water and position 5 of dUMP, occurrence of reactions other than a methyl-group transfer during the interaction of the enzyme with its 2 substrates
-
-
-
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
-
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
-
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
-
additional information
?
-
A6M9A2, -
recombinant protein is able to bind its own RNA
-
-
-
additional information
?
-
-
the enzyme is specifically bound with its cognate mRNA in vitro and in vivo
-
-
-
additional information
?
-
-
thymidylate synthase form ThyX has no activity in Corynebacterium glutamicum
-
-
-
additional information
?
-
Lactobacillus casei TS N229D
-
dCMP is no substrate, exception mutant TS N229D
-
-
-
additional information
?
-
Escherichia coli EM 20031 K12
-
nucleotides with large substituents on the 2' position are no substrates, enzyme catalyzes the exchange of a hydrogen atom between water and position 5 of dUMP, occurrence of reactions other than a methyl-group transfer during the interaction of the enzyme with its 2 substrates
-
-
-
additional information
?
-
Corynebacterium glutamicum NCHU 87078
-
thymidylate synthase form ThyX has no activity in Corynebacterium glutamicum
-
-
-
additional information
?
-
Escherichia coli K12
-
nucleotides with large substituents on the 2' position are no substrates, enzyme catalyzes the exchange of a hydrogen atom between water and position 5 of dUMP, occurrence of reactions other than a methyl-group transfer during the interaction of the enzyme with its 2 substrates
-
-
-
additional information
?
-
Escherichia coli K12
-
-
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
thymidylate synthase is the third enzyme in the methylene tetrahydrofolate cycle besides dihydrofolate reductase and serine hydroxymethyltransferase, in many organisms, thymidylate synthase is the only de novo source for dTMP required for DNA synthesis
-
-
?
5,10-methylenetetrahydrofolate + deoxyuridine monophosphate
7,8-dihydrofolate + deoxythymidine monophosphate
show the reaction diagram
B5U9U8, -
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P0CI79
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P0A884
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Abies sp.
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P45351
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Trypanosoma rhodesiense
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P04818
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P13100
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
P45351
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
P04818
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-, P67044
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
inhibition of thymidylate synthase or of DHFR leads to thymineless death of eukaryotic organisms
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
it is a key enzyme for the synthesis of the DNA-specific nucleotide thymidylate
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
thymidylate synthase catalyses the only de novo pathway to produce thymidylate for DNA replication and repair
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
thymidylate synthase is a key enzyme in the de novo synthesis of dTMP
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
thymidylate synthase is an essential enzyme for de novo synthesis of thymidylate (dTMP), a precursor for DNA synthesis
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
A6M9A2, -
thymidylate synthase is essential for de novo synthesis of dTMP and is a key enzyme involved in DNA synthesis and transcriptional regulation of organisms
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
show the reaction diagram
-
TS is a key enzyme in folate metabolism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + TMP
show the reaction diagram
-
during TS inhibition, TMP levels decrease with a subsequent increase in dUTP
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Lactobacillus casei TS N229D
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli EM 20031 K12
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli K12
-
-
-
-
?
N5,N10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + TMP
show the reaction diagram
-
during thymidylate synthase inhibition, TMP levels decrease with a subsequent increase in dUTP
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
show the reaction diagram
Escherichia coli R2
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
additional information
?
-
A6M9A2, -
recombinant protein is able to bind its own RNA
-
-
-
COFACTOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
(+)-methylenetetrahydrofolate
-
-
(+)-methylenetetrahydrofolate
-
-
(6R)-5,10-methylene-5,6,7,8-tetrahydrofolate
-
-
methenyltetrahydropteroylglutamate
-
-
N5,N10-methylenetetrahydrofolate
-
-
N5,N10-methylenetetrahydrofolate
Acinetobacter baumannii, Aeromonas hydrophila, Ascaris suum, Aspergillus clavatus, Aspergillus fumigatus, Bacillus amyloliquefaciens, Bacillus anthracis, Bacillus cereus, Bacillus licheniformis, Bacillus weihenstephanensis, Bacteroides fragilis, Bacteroides thetaiotaomicron, Bartonella bacilliformis, Bartonella henselae, Bartonella quintana, Bordetella bronchiseptica, Bordetella parapertussis, Bordetella pertussis, Brucella abortus, Brucella melitensis, Brucella suis, Burkholderia ambifaria, Burkholderia dolosa, Burkholderia mallei, Burkholderia multivorans, Burkholderia pseudomallei, Burkholderia vietnamiensis, Candida albicans, Candida glabrata, Chaetomium globosum, Chromobacterium violaceum, Clostridium difficile, Coccidioides immitis, Comamonas testosteroni, Corynebacterium diphtheriae, Corynebacterium jeikeium, Coxiella burnetii, Cryptococcus neoformans, Cryptosporidium hominis, Cryptosporidium parvum, Debaryomyces hansenii, Emericella nidulans, Encephalitozoon cuniculi, Enterobacter sp., Enterococcus faecalis, Enterococcus faecium, Francisella tularensis, Fusobacterium nucleatum, Haemophilus ducreyi, Haemophilus influenzae, Human herpesvirus 1, Legionella pneumophila, Leishmania amazonensis, Leishmania braziliensis, Leishmania donovani, Leishmania infantum, Leishmania major, Leishmania tropica, Listeria monocytogenes, Mycobacterium avium, Mycobacterium bovis, Mycobacterium leprae, Mycobacterium tuberculosis, Mycobacterium ulcerans, Mycoplasma genitalium, Mycoplasma penetrans, Mycoplasma pneumoniae, Neisseria gonorrhoeae, Neisseria meningitidis, Neosartorya fischeri, Nocardia farcinica, Novosphingobium aromaticivorans, Pasteurella multocida
-
-
N5,N10-methylenetetrahydrofolate
-
-
N5,N10-methylenetetrahydrofolate
-
-
N5,N10-methylenetetrahydrofolate
-
-
N5,N10-methylenetetrahydrofolate
C6GJB8, -
-
N5,N10-methylenetetrahydrofolate
Q8QTF3, -
-
N5,N10-methylenetetrahydrofolate
-
-
N5,N10-methylenetetrahydrofolate
-
-
N5,N10-methylenetetrahydrofolate
-
-
N5,N10-methylenetetrahydrofolate
-
-
N5,N10-methylenetetrahydrofolate
-
-
NADPH
-
absolute requirement
methylenetetrahydrofolate
-
-
additional information
-
the enzyme is FAD-independent
-
METALS and IONS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
Mg2+
-
requirement depending upon the buffer
Mg2+
-
in Tris-acetate buffers 10 mM enhances enzyme activity by some 30%
Mg2+
-
high requirement
Na+
-
stimulates activity
INHIBITORS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
(+)tetrahydropteroylglutamate
-
-
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
(6R)-tetrahydropteroylglutamate
-
-
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo(f)quinazolin-9-yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
-
BW1843U89, U89, distorts the thymidylate synthase active site
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9 yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
C6GJB8, -
-
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9-yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
Q8QTF3, -
-
(S)-2-(5-(((1,2-dihydro3-methyl-1-oxobenzo[f]quinazolin-9-yl)methyl)amino)-1-oxo-2-isoindolinyl)glutaric acid
-
BW1843U89
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
Acinetobacter baumannii, Aeromonas hydrophila, Ascaris suum, Aspergillus clavatus, Aspergillus fumigatus, Bacillus amyloliquefaciens, Bacillus anthracis, Bacillus cereus, Bacillus licheniformis, Bacillus weihenstephanensis, Bacteroides fragilis, Bacteroides thetaiotaomicron, Bartonella bacilliformis, Bartonella henselae, Bartonella quintana, Bordetella bronchiseptica, Bordetella parapertussis, Bordetella pertussis, Brucella abortus, Brucella melitensis, Brucella suis, Burkholderia ambifaria, Burkholderia dolosa, Burkholderia mallei, Burkholderia multivorans, Burkholderia pseudomallei, Burkholderia vietnamiensis, Candida albicans, Candida glabrata, Chaetomium globosum, Chromobacterium violaceum, Clostridium difficile, Coccidioides immitis, Comamonas testosteroni, Corynebacterium diphtheriae, Corynebacterium jeikeium, Coxiella burnetii, Cryptococcus neoformans, Cryptosporidium hominis, Cryptosporidium parvum, Debaryomyces hansenii, Emericella nidulans, Encephalitozoon cuniculi, Enterobacter sp., Enterococcus faecalis, Enterococcus faecium, Francisella tularensis, Fusobacterium nucleatum, Haemophilus ducreyi, Haemophilus influenzae, Human herpesvirus 1, Legionella pneumophila, Leishmania amazonensis, Leishmania braziliensis, Leishmania donovani, Leishmania infantum, Leishmania major, Leishmania tropica, Listeria monocytogenes, Mycobacterium avium, Mycobacterium bovis, Mycobacterium leprae, Mycobacterium tuberculosis, Mycobacterium ulcerans, Mycoplasma genitalium, Mycoplasma penetrans, Mycoplasma pneumoniae, Neisseria gonorrhoeae, Neisseria meningitidis, Neosartorya fischeri, Nocardia farcinica, Novosphingobium aromaticivorans, Pasteurella multocida
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
P13922
-
1,3-propanediphosphonic acid
-
allosteric inhibitor of human thymidylate synthase; stabilizes an inactive conformer of loop 181-197. Mixed inhibitor of dUMP, uncompetitive inhibitor versus methylenetetrahydrofolate below 0.00025 mM, noncompetitive above 0.001 mM, respectively. 1,3-Propanediphosphonic acid shows positive cooperativity with antifolate inhibitor ZD9331. It leads to the formation of enzyme tetramers, but not of higher oligomers
1-(2'-deoxyribosyl)8-azapurin-2-one 5'-monophosphate
-
-
1-(beta-D-2'-deoxyribofuranosyl)1,6-dihydro-8-azapurin-2(3H,6H)-one 5'-monophosphate
-
-
1-(beta-D-2'-Deoxyribofuranosyl)8-azapurin-2-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate
-
-
1-ethyl-3-dimethylaminopropyl carbodiimide
-
-
1-phenyl-3-(3-dimethylaminopropyl) carbodiimide
-
-
1-phenyl-3-(3-trimethylaminopropyl) carbodiimide
-
-
10-formyl folic acid
-
-
10-formyl-5,8-dideazafolate
-
-
10-formyldihydropteroylglutamate
-
-
10-formyldihydropteroylheptaglutamate
-
-
-
10-formyldihydropteroylpentaglutamate
-
-
10-formyltetrahydrofolate
-
-
10-Formyltetrahydrofolylheptaglutamate
-
-
10-Formyltetrahydrofolylmonoglutamate
-
-
10-formyltetrahydropteroylheptaglutamate
-
-
10-formyltetrahydropteroylmonoglutamate
-
-
10-formyltetrahydropteroylpolyglutamate
-
-
10-methenyldihydropteroylpentaglutamate
-
-
-
10-methenyltetrahydropteroylheptaglutamate
-
-
-
10-methylfolate
-
-
-
10-propargyl-5,8-dideazafolate
-
PDDF
-
10-propargyl-5,8-dideazafolate
-
PDDF, folate-like TS inhibitor
-
10-propargyl-5,8-dideazafolate
-
i.e. PDDF. Dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
-
10-propargyl-5,8-dideazafolate
-
i.e. PDDF. Dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
-
10-propargyl-5,8-dideazafolate
-
i.e. PDDF. Dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
-
10-propargyl-5,8-dideazafolate
C6GJB8, -
-
-
10-propargyl-5,8-dideazafolate
Q8QTF3, -
-
-
10-propargyl-5,8-dideazafolate
-
-
-
10-propargyl-5,8-dideazafolate
-
-
-
1843U89
-, P67044
i.e. (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, folate-based inhibitor
2',5-difluoro-ara-UMP
-
slow-binding (time-dependent) inhibitor
2'-deoxy-2',2'-difluorouridine 5'-dihydrogen
-
classic inhibitor (no time dependence of inhibition observed)
2'-deoxy-5-fluorouridine 5'-phosphate
-
-
2'-Deoxyuridine
-
-
2'-fluoro-ara-UMP
-
classic inhibitor (no time dependence of inhibition observed)
2,4-diamino pteridine
-
-
2,4-diamino quinazoline antifolate
-
-
2-amino-4-hydroxyquinazoline
-
-
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
-
-
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
2-hydroxyethyl disulfide
-
-
3,3-bis(4-methoxyphenyl)-1H,3H-benzo[de]isochromen-1-one
-
induces apoptotic cell death in SK-MEL-2 and SK-MEL-28 melanoma cell lines, mediated by downregulation of Bcl-2 protein level and PARP cleavage, and independent of p53 and Bax. Pan-caspases inhibitor Z-VAD-FMK blocks the effect
3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
Acinetobacter baumannii, Aeromonas hydrophila, Ascaris suum, Aspergillus clavatus, Aspergillus fumigatus, Bacillus amyloliquefaciens, Bacillus anthracis, Bacillus cereus, Bacillus licheniformis, Bacillus weihenstephanensis, Bacteroides fragilis, Bacteroides thetaiotaomicron, Bartonella bacilliformis, Bartonella henselae, Bartonella quintana, Bordetella bronchiseptica, Bordetella parapertussis, Bordetella pertussis, Brucella abortus, Brucella melitensis, Brucella suis, Burkholderia ambifaria, Burkholderia dolosa, Burkholderia mallei, Burkholderia multivorans, Burkholderia pseudomallei, Burkholderia vietnamiensis, Candida albicans, Candida glabrata, Chaetomium globosum, Chromobacterium violaceum, Clostridium difficile, Coccidioides immitis, Comamonas testosteroni, Corynebacterium diphtheriae, Corynebacterium jeikeium, Coxiella burnetii, Cryptococcus neoformans, Cryptosporidium hominis, Cryptosporidium parvum, Debaryomyces hansenii, Emericella nidulans, Encephalitozoon cuniculi, Enterobacter sp., Enterococcus faecalis, Enterococcus faecium, Francisella tularensis, Fusobacterium nucleatum, Haemophilus ducreyi, Haemophilus influenzae, Human herpesvirus 1, Legionella pneumophila, Leishmania amazonensis, Leishmania braziliensis, Leishmania donovani, Leishmania infantum, Leishmania major, Leishmania tropica, Listeria monocytogenes, Mycobacterium avium, Mycobacterium bovis, Mycobacterium leprae, Mycobacterium tuberculosis, Mycobacterium ulcerans, Mycoplasma genitalium, Mycoplasma penetrans, Mycoplasma pneumoniae, Neisseria gonorrhoeae, Neisseria meningitidis, Neosartorya fischeri, Nocardia farcinica, Novosphingobium aromaticivorans, Pasteurella multocida
-
-
3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
P13922
-
3-beta-D-ribofuranosylmaleimide
-
showdomycin
3-beta-D-ribofuranosylmaleimide 5'-phosphate
-
showdomycin 5'-phosphate
4-amino-N10-methylfolic acid
-
-
5'-CGCGGTACGGACACCGCGCG-3'
-
targets the TS mRNA translation start site TSS and increases the thymidylate synthase gene transcription in HeLa cell
-
5,10-methylenetetrahydrofolate
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5-bromo-2'-deoxyuridylic acid
-
-
5-bromo-N4-hydroxy-2'-deoxycytidine
-
-
5-bromoacetamido-5'-deoxythymidine
-
-
5-chloro-N4-hydroxy-2'-deoxycytidine
-
-
5-chloroacetamido-5'-deoxythymidine
-
-
5-fluoro-2'-deoxyuridine
-
comparison with inhibitory effect of FdUMP[10] and 5-fluorouraci
5-fluoro-2'-deoxyuridine 5'-(p-aminophenyl phosphate)
-
-
5-fluoro-2'-deoxyuridine 5'-(p-aminophenyl phosphate)
-
-
5-fluoro-2'-deoxyuridine 5'-monophosphate
-
-
5-fluoro-2'-deoxyuridine 5'-monophosphate
-, P67044
FdUMP
5-fluoro-2'-deoxyuridine monophosphate
-
-
-
5-fluoro-2'-deoxyuridine-5'-monophosphate
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
very strong inhibition, pseudo-noncompetitive
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-Fluoro-2-deoxyuridine
-
FUdR
5-fluoro-dUMP
-
-
5-fluoro-dUMP[10]
-
a 10-mer of 5-fluoro-dUMP, a suicide inhibitor of thymidylate synthase, designed to bypass resistance to 5-fluorouracil, acts as a pro-drug of 5-fluoro-dUMP
5-fluorodeoxyuridine
-
5-FUdR, TS-targeting chemotherapeutic agent
5-fluorodeoxyuridine
-
-
5-fluorodeoxyuridine
-
forms an inhibitory, ternary covalent complex with the enzyme
5-fluoropyrimidine-2,4(1H,3H)-dione
-
-
5-Fluorouracil
-
-
5-Fluorouracil
-
but a major mechanism of resistance to 5-fluorouracil is overexpression of thymidylate synthase
5-Fluorouracil
-
5-FU
5-Fluorouracil
-
5-FU, TS-targeting chemotherapeutic agent
5-Fluorouracil
-
WiDr cells: 0.005 mM inhibits growth to 22%, inhibition cannot be potentiated by leucovorin but is rescued by uridine, 0.025 mM inhibits growth to 10%, inhibition can be rescued badly by uridine to an value of 31%, SW-948 and HT-29 cells: 0.005 mM shows an antiproliferative activity that is not affected by leucovorine addition and can be rescued by uridine, 0.1 mM shows a complete inhibition that cannot be rescued by uridine
5-Fluorouracil
-
0.001 mM inhibits growth to 13%, inhibition can be rescued by uridine, 0.005 mM inhibits growth completely, inhibition cannot be rescued by uridine
5-Fluorouracil
-
transfection with p53 induces resistance to 5-fluorouracil
5-Fluorouracil
-
; comparison with inhibitory effect of FdUMP[10] and 5-fluoro-2'-deoxyuridine
5-fluorouridine
-
-
5-Formyl-2'-deoxyuridylic acid
-
-
5-Formyl-2'-deoxyuridylic acid
-
-
5-Formyl-2'-deoxyuridylic acid
-
-
5-haloacetamido-5'-deoxythymidine
-
-
5-hydroseleno-2'-deoxyuridylic acid
-
-
5-hydroxy-methyl-2'-deoxyuridine 5'-monophosphate
-
-
5-iodo-2'-deoxyuridylic acid
-
-
5-iodoacetamido-5'-deoxythymidine
-
-
5-iodoacetamidomethyl-2'-deoxyuridine 5'-phosphate
-
-
5-Mercapto-2'-deoxyuridylic acid
-
-
5-Mercapto-2'-deoxyuridylic acid
-
possesses antitumor activity against Ehrlich ascites cells
5-Mercapto-2'-deoxyuridylic acid
-
-
5-Nitro-2'-deoxyuridine 5'-monophosphate
-
-
5-nitro-2'-deoxyuridylic acid
-
-
5-trifluoromethyl-2'-deoxyuridine 5'-monophosphate
-
-
5-trifluoromethyl-2'-deoxyuridylic acid
-
-
6-bromo-3,3-bis(3-chloro-4-hydroxyphenyl)-1H,3H-benzo[de]isochromen-1-one
-
induces apoptotic cell death in SK-MEL-2 and SK-MEL-28 melanoma cell lines, mediated by downregulation of Bcl-2 protein level and PARP cleavage, and independent of p53 and Bax. Pan-caspases inhibitor Z-VAD-FMK blocks the effect
6-chloro-3,3-bis(4-hydroxyphenyl)-1H,3H-benzo[de]isochromen-1-one
-
induces apoptotic cell death in SK-MEL-2 and SK-MEL-28 melanoma cell lines, mediated by downregulation of Bcl-2 protein level and PARP cleavage, and independent of p53 and Bax. Pan-caspases inhibitor Z-VAD-FMK blocks the effect
8-azapurinone deoxyribonucleoside 5'-phosphate
-
-
-
antifolate
B5U9U8, -
inhibits activitiy of bifunctional DHFR-TS enzyme
-
Arabinouridylate
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
Acinetobacter baumannii, Aeromonas hydrophila, Ascaris suum, Aspergillus clavatus, Aspergillus fumigatus, Bacillus amyloliquefaciens, Bacillus anthracis, Bacillus cereus, Bacillus licheniformis, Bacillus weihenstephanensis, Bacteroides fragilis, Bacteroides thetaiotaomicron, Bartonella bacilliformis, Bartonella henselae, Bartonella quintana, Bordetella bronchiseptica, Bordetella parapertussis, Bordetella pertussis, Brucella abortus, Brucella melitensis, Brucella suis, Burkholderia ambifaria, Burkholderia dolosa, Burkholderia mallei, Burkholderia multivorans, Burkholderia pseudomallei, Burkholderia vietnamiensis, Candida albicans, Candida glabrata, Chaetomium globosum, Chromobacterium violaceum, Clostridium difficile, Coccidioides immitis, Comamonas testosteroni, Corynebacterium diphtheriae, Corynebacterium jeikeium, Coxiella burnetii, Cryptococcus neoformans, Cryptosporidium hominis, Cryptosporidium parvum, Debaryomyces hansenii, Emericella nidulans, Encephalitozoon cuniculi, Enterobacter sp., Enterococcus faecalis, Enterococcus faecium, Francisella tularensis, Fusobacterium nucleatum, Haemophilus ducreyi, Haemophilus influenzae, Human herpesvirus 1, Legionella pneumophila, Leishmania amazonensis, Leishmania braziliensis, Leishmania donovani, Leishmania infantum, Leishmania major, Leishmania tropica, Listeria monocytogenes, Mycobacterium avium, Mycobacterium bovis, Mycobacterium leprae, Mycobacterium tuberculosis, Mycobacterium ulcerans, Mycoplasma genitalium, Mycoplasma penetrans, Mycoplasma pneumoniae, Neisseria gonorrhoeae, Neisseria meningitidis, Neosartorya fischeri, Nocardia farcinica, Novosphingobium aromaticivorans, Pasteurella multocida
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
P13922
-
BGC 9331
-
treatment results in concentration-dependent increase in thymidine uptake in FR-positive epidermoid KB cells and in increase of membrane-associated equilibrative nucleoside transporter type 1 levels. Tumor [18F]-fluorothymidine accumulation in KB xenografts increases by more than 2fold with maximal levels at 1 to 4 hours and 4 to 24 hours after drug treatment. Quantitiative changes in tumor [18F]-fluorothymidine uptake are associated with increased tumor dUrd levels. BGC 9331 induces accumulation of [18F]-fluorothymidine uptake in the intestine
BGC 945
-
alpha-folate receptor targeted antifolate TS inhibitor; cyclopenta[g]quinazoline-based inhibitor. Treatment results in concentration-dependent increase in thymidine uptake in FR-positive epidermoid KB cells and in increase of membrane-associated equilibrative nucleoside transporter type 1 levels. Tumor [18F]-fluorothymidine accumulation in KB xenografts increases by more than 2fold with maximal levels at 1 to 4 hours and 4 to 24 hours after drug treatment. Quantitiative changes in tumor [18F]-fluorothymidine uptake are associated with increased tumor dUrd levels
bromo-2'-deoxyuridine
-
-
bromodeoxyuridine
-
-
capecitabine
-
prodrug of 5-fluorouracil
chloro-2'-deoxyuridine
-
-
Chloroacetamide
-
-
cytosine arabinoside
-
-
deaza-aminopterin
-
-
diglutamate
-
-
dihydropteroylglutamate
-
-
dihydropteroylhexaglutamate
-
-
dihydropteroylpentaglutamate
-
-
dihydropteroyltriglutamate
-
-
dithiophosphate
-
-
ethyl methanesulfonate
-
-
ethylene glycol
-
-
FdUMP[10]
-
multimer of 5-fluoro-2'-deoxyuridine 5'-monophosphate, inhibits cell growth with greater potency than 5-fluorouracil and 5-fluoro-2'-deoxyuridine
FdUSSO3
-
-
-
fluorodeoxyuridine monophosphate
-
-
-
fluorodeoxyuridine monophosphate
-
-
-
fluoroorotic acid
-
-
folic acid oligoglutamate
-
-
-
gefitinib
-
inhibits the expression of the transcription factor E2F-1, resulting in a down-regulation of thymidylate synthase at the mRNA and protein level; inhibits the expression of the transcription factor E2F-1, resulting in the down-regulation of thymidylate synthase at the mRNA and protein levels
glyceraldehyde 3-phosphate
-
-
GW1843U89
-
-
GW1843U89
-
direct folate-based inhibitor
hydroxymethyl-2'-deoxyuridine
-
-
Hydroxyurea
-
supresses thymidilate synthase in growing algae, but no effect on purified enzyme
iodo-2'-deoxyuridine
-
-
iodoacetate
-
-
Iododeoxyuridine
-
-
N,O-didansyl-L-tyrosine
Acinetobacter baumannii, Aeromonas hydrophila, Ascaris suum, Aspergillus clavatus, Aspergillus fumigatus, Bacillus amyloliquefaciens, Bacillus anthracis, Bacillus cereus, Bacillus licheniformis, Bacillus weihenstephanensis, Bacteroides fragilis, Bacteroides thetaiotaomicron, Bartonella bacilliformis, Bartonella henselae, Bartonella quintana, Bordetella bronchiseptica, Bordetella parapertussis, Bordetella pertussis, Brucella abortus, Brucella melitensis, Brucella suis, Burkholderia ambifaria, Burkholderia dolosa, Burkholderia mallei, Burkholderia multivorans, Burkholderia pseudomallei, Burkholderia vietnamiensis, Candida albicans, Candida glabrata, Chaetomium globosum, Chromobacterium violaceum, Clostridium difficile, Coccidioides immitis, Comamonas testosteroni, Corynebacterium diphtheriae, Corynebacterium jeikeium, Coxiella burnetii, Cryptococcus neoformans, Cryptosporidium hominis, Cryptosporidium parvum, Debaryomyces hansenii, Emericella nidulans, Encephalitozoon cuniculi, Enterobacter sp., Enterococcus faecalis, Enterococcus faecium, Francisella tularensis, Fusobacterium nucleatum, Haemophilus ducreyi, Haemophilus influenzae, Human herpesvirus 1, Legionella pneumophila, Leishmania amazonensis, Leishmania braziliensis, Leishmania donovani, Leishmania infantum, Leishmania major, Leishmania tropica, Listeria monocytogenes, Mycobacterium avium, Mycobacterium bovis, Mycobacterium leprae, Mycobacterium tuberculosis, Mycobacterium ulcerans, Mycoplasma genitalium, Mycoplasma penetrans, Mycoplasma pneumoniae, Neisseria gonorrhoeae, Neisseria meningitidis, Neosartorya fischeri, Nocardia farcinica, Novosphingobium aromaticivorans, Pasteurella multocida
-
-
N,O-didansyl-L-tyrosine
P13922
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
-
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydrothieno(2,3-d)pyrimidin-5-yl)sulfanyl)benzoyl)-L-glutamic acid
-
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
-
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamyl-gamma-glutamyl-gamma-glutamylglutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamylglutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
-
-
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
-
-
N-ethylmaleimide
-
-
N-ethylmaleimide
-
-
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
-
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
-
-
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme; dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
potent inhibitor of thymidylate synthase
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N10-formyltetrahydrofolate
-
-
N4-hydroxy-2'-deoxycytidine
-
-
N4-hydroxy-5-methyl-2'-deoxycytidine
-
-
N5-formiminotetrahydropteroyltriglutamate
-
-
N5-formyltetrahydropteroyloligoglutamate
-
-
nolatrexed
-
transfection with p53 induces resistance to nolatrexed
nolatrexed
-
-
novobiocin
-
coumarin antibiotic produced by Streptomyces nivens, at 10 mM concentration the self-splicing of primary transcripts is inhibited by about 5%, at 40 mM concentration the splicing rate is inhibited by about 50%. The splicing inhibition is strongly dependent on Mg2+
o-propargyl-5,8-dideazafolate
-
-
-
OSI-7904L
-
a liposomal thymidylate synthase inhibitor, a liposomal formulation of OSI-7904 (S)-2-(5-((1,2-dihydro-3-methyl-1-oxobenzo(f)quinazolin-9-yl)methyl)amino-1-oxo-2-isoindolynl)-glutaric acid, administered in combination with oxaliplatin every 21 days in patients with advanced colorectal carcinoma; treatment of patients with advanced colorectal carcinoma, in combination with oxaliplatin. At the highest dose level of OSI-7904L 9 mg/m2, oxaliplatin 130 mg/m2, one of nine patients experienced dose-limiting toxicity of grade 3 oral mucositis with cycle 1 and five further patients required dose reductions. The toxicity profile of stomatitis, diarrhea, nausea, fatigue, sensory neuropathy and skin rash was consistent with that expected for a thymidylate synthase inhibitor/oxaliplatin combination regimen. High interpatient variability with no detectable interaction between OSI-7904L and oxaliplatin
p-chloromercuribenzoate
-
-
pemetrexed
-
TS-targeting chemotherapeutic agent
pemetrexed
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
pemetrexed
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
pemetrexed
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
pemetrexed
-
transfection with p53 induces resistance to pemetrexed
pemetrexed
-
direct folate-based inhibitor; inhibitory to cell growth even in cell lacking thymidylate synthase activity
Phenylglyoxal
-
-
Procion blue
-
-
propylene diphosphonate
-
mixed competitive-noncompetitive inhibitor with respect to dUMP
-
pteroyldiglutamate
-
-
Pteroylheptaglutamate
-
-
pteroylhexaglutamate
-
-
pteroylhexaglutamate
-
-
pteroylhexaglutamate
-
-
pteroylmonoglutamate
-
-
pteroylpentaglutamate
-
-
pteroylpolyglutamate
-
-
pteroylpolyglutamate
-
-
pteroyltetraglutamate
-
-
Pteroyltriglutamate
-
-
pyridoxal 5'-phosphate
-
-
raltitrexed
-
RTX, a folate analog that is a specific inhibitor of TS; treatment can stimulate accurate recombination events in human cells. Gene conversions not associated with crossovers are specifically enhanced severalfold. Recombination events provoked by a double-strand break are not impacted by treatment with raltitrexed, nor is error-prone double-strand break repair via nonhomologous end-joining
raltitrexed
-
TS-targeting chemotherapeutic agent
raltitrexed
-
transfection with p53 induces resistance to raltitrexed
raltitrexed
-
direct folate-based inhibitor
tetrahydrohomofolate
-
-
tetrahydromethotrexate
-
-
tetrahydromethotrexate
-
-
tetrahydromethotrexate
-
-
thiophosphate
-
-
thymidine phosphate
-
product inhibition
thymidine phosphate
-
-
thymidine phosphate
-
-
thymidine phosphate
-
-
thymidine phosphate
-
-
thymidine phosphate
-
-
trifluoromethyldeoxyuridine 5'-monophosphate
-
-
trifluoromethyldeoxyuridine 5'-monophosphate
-
-
trifluoromethyldeoxyuridine 5'-monophosphate
-
-
trimethoprim
-
-
UDP-glucuronate
-
-
vanoxonin-vanadium
-
-
ZD9331
-
antifolate inhibitor, shows positive cooperativity with 1,3-propanediphosphonic acid
additional information
-
5FU-LV, combination of 5-fluorouracil and leucovorin
-
additional information
-
combination of 5-FU and leucovorin, enhances the inhibition of thymidylate synthase, 0.001 mM inhibits growth to only 1%, inhibition can be rescued by uridine to an almost normal value of 83%
-
additional information
-
combination of leucovorin and 5-fluorouracil 5FU-LV, IC50 0.00016 (FM3A/0 cell)
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
(NH4)2SO4
-
10 mM, relative activity 108%
2,3-Dimercaptopropanol
-
absolute requirement for a thiol, synthetase shows greatly dimished activity in absence
ATP
-
0.1 mM, relative activity 102%
beta-mercaptoethanol
-
-
beta-mercaptoethanol
-
essential for maximum activity
dithiothreitol
-
-
dithiothreitol
-
thiols enhances enzyme activity
dithiothreitol
-
maximal catalytic activity only in presence of sulfhydryl compounds
dithiothreitol
-
enzyme activity is stimulated 2fold by 8-20 mM
dithiothreitol
-
-
EDTA
-
5.0 mM, relative activity 103%
KM VALUE [mM]
KM VALUE [mM] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.014
-
(+-)5,10-methylene-5,6,7,8-tetrahydrofolate
-
-
0.012
-
(+-)methylenetetrahydrofolate
-
in presence of 10 mM Mg2+
0.032
-
(+-)methylenetetrahydrofolate
-
-
0.07
-
(-)-5,10-methylene-tetrahydropteroylglutamate
-
-
0.061
-
(6S)-tetrahydropteroylglutamate
-
-
0.025
-
(l)-tetrahydropteroyltriglutamate
-
-
0.3
-
(R)-5,10-methylene-5,6,7,8-tetrahydrofolate
-
30fold higher than wild-type thymidylate synthase
0.3
-
(R)-5,10-methylenetetrahydrofolate
-
mutant K48Q
0.15
-
2'-deoxycytidine 5'-monophosphate
-
mutant TS N229D
0.0015
-
2'-deoxyuridine 5'-monophosphate
-
-
0.0007
-
2'-deoxyuridylate
P04818
mutant 362(T51S,K82Q,N171S)
0.001
-
2'-deoxyuridylate
P04818
mutant Y258F
0.0011
-
2'-deoxyuridylate
-
wild-type
0.0011
-
2'-deoxyuridylate
P04818
mutant 302(T53S,Y258F)
0.0012
-
2'-deoxyuridylate
-
-
0.0012
-
2'-deoxyuridylate
-
mutant Y4F
0.0012
-
2'-deoxyuridylate
-
wild-type
0.0013
-
2'-deoxyuridylate
-
native enzyme
0.0014
-
2'-deoxyuridylate
-
mutant Y4I, Y4V
0.0015
-
2'-deoxyuridylate
-
mutant P254G
0.0018
-
2'-deoxyuridylate
-
-
0.0018
-
2'-deoxyuridylate
-
mutant P254F
0.002
-
2'-deoxyuridylate
-
recombinant enzyme
0.002
-
2'-deoxyuridylate
P04818
wild type
0.0026
-
2'-deoxyuridylate
P45351
-
0.0026
-
2'-deoxyuridylate
P04818
mutant T51S
0.0027
-
2'-deoxyuridylate
-
mutant P254S
0.003
-
2'-deoxyuridylate
-
mutant Y4H
0.00315
-
2'-deoxyuridylate
-
-
0.0033
-
2'-deoxyuridylate
-
-
0.0034
-
2'-deoxyuridylate
-
-
0.0034
-
2'-deoxyuridylate
-
mutant P254D
0.0036
-
2'-deoxyuridylate
-
-
0.00365
-
2'-deoxyuridylate
-
-
0.0037
-
2'-deoxyuridylate
-
-
0.00378
-
2'-deoxyuridylate
-
-
0.004
-
2'-deoxyuridylate
-
-
0.005
-
2'-deoxyuridylate
-
-
0.005
-
2'-deoxyuridylate
-
wild-type
0.0051
-
2'-deoxyuridylate
-
in presence of 10 mM Mg2+
0.0053
-
2'-deoxyuridylate
-
mutant S167A
0.0057
-
2'-deoxyuridylate
-
-
0.0063
-
2'-deoxyuridylate
-
-
0.0063
-
2'-deoxyuridylate
-
mutant D221S
0.0063
-
2'-deoxyuridylate
-
-
0.0068
-
2'-deoxyuridylate
-
-
0.0068
-
2'-deoxyuridylate
-
-
0.0075
-
2'-deoxyuridylate
-
-
0.009
-
2'-deoxyuridylate
-
-
0.0092
-
2'-deoxyuridylate
-
-
0.01
-
2'-deoxyuridylate
-
-
0.01
-
2'-deoxyuridylate
-
-
0.0104
-
2'-deoxyuridylate
-
-
0.011
-
2'-deoxyuridylate
-
mutant D221E
0.011
-
2'-deoxyuridylate
-
-
0.014
-
2'-deoxyuridylate
-
Ehrlich ascites carcinoma cells
0.015
-
2'-deoxyuridylate
-
mutant D221C
0.015
-
2'-deoxyuridylate
-
-
0.017
-
2'-deoxyuridylate
-
mutant TS N229C
0.018
-
2'-deoxyuridylate
-
phage infected E. coli
0.02
-
2'-deoxyuridylate
-
less purified enzyme
0.03
-
2'-deoxyuridylate
-
phage infected E. coli
0.0308
-
2'-deoxyuridylate
-
-
0.0339
-
2'-deoxyuridylate
-
mutant S167G
0.037
-
2'-deoxyuridylate
-
Ehrlich ascites carcinoma cells
0.0417
-
2'-deoxyuridylate
-
mutant S167T
0.05
-
2'-deoxyuridylate
-
mutant TS N229D
0.0714
-
2'-deoxyuridylate
-
-
0.0981
-
2'-deoxyuridylate
-
mutant S167C
0.0137
-
2'-deoxyuridylate 5'-dithiophosphate
-
-
0.0155
-
2'-deoxyuridylate 5'-dithiophosphate
-
-
0.00632
-
2'-deoxyuridylate 5'-thiophosphate
-
-
0.037
-
2'-deoxyuridylate 5'-thiophosphate
-
-
0.11
-
2'-fluoro-2'-deoxyuridine 5'-phosphate
-
-
0.113
-
2'-fluoro-2'-deoxyuridine 5'-phosphate
-
-
0.00068
-
5,10-formyltetrahydropteroylheptaglutamate
-
-
0.00074
-
5,10-methenyltetrahydropteroylpentaglutamate
-
-
0.0015
-
5,10-methylenetetrahydrofolate
-
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 25C
0.004
-
5,10-methylenetetrahydrofolate
-, P67044
22C
0.0134
-
5,10-methylenetetrahydrofolate
Q8QTF3, -
at 30C
0.0135
-
5,10-methylenetetrahydrofolate
C6GJB8, -
at 30C
0.039
-
5,10-methylenetetrahydrofolate
-
-
0.043
-
5,10-methylenetetrahydrofolate
-
-
0.0524
-
5,10-methylenetetrahydrofolate
-
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 25C
0.07
-
5,10-methylenetetrahydrofolate
-, P67044
; 22C
0.185
-
5,10-methylenetetrahydrofolate
-
-
0.031
-
5,10-methylenetetrahydropteroylglutamate
-
-
0.0022
-
5,10-methylenetetrahydropteroylpentaglutamate
-
-
0.0097
-
5-bromo-2'-deoxyuridine
-
wild-type
0.0723
-
5-bromo-2'-deoxyuridine
-
mutant S167A
0.514
-
5-bromo-2'-deoxyuridine
-
mutant S167G
0.0057
-
5-bromo-2'-deoxyuridylate
-
wild-type
0.0057
-
5-bromo-2'-deoxyuridylate
-
-
0.02
-
5-bromo-2'-deoxyuridylate
-
mutant D221A
0.02
-
5-bromo-2'-deoxyuridylate
-
-
0.025
-
5-bromo-2'-deoxyuridylate
-
mutant D221C
0.025
-
5-bromo-2'-deoxyuridylate
-
-
0.027
-
5-bromo-2'-deoxyuridylate
-
mutant D221S
0.027
-
5-bromo-2'-deoxyuridylate
-
-
0.045
-
5-bromo-2'-deoxyuridylate
-
mutant D221N
0.045
-
5-bromo-2'-deoxyuridylate
-
-
0.046
-
5-bromo-2'-deoxyuridylate
-
mutant D221E
0.046
-
5-bromo-2'-deoxyuridylate
-
-
0.003
-
deoxyuridine phosphate
-, P67044
22C
0.004
-
deoxyuridine phosphate
-, P67044
22C
0.00085
-
dUMP
-
mutant enzyme A191K, at 37C
0.00096
-
dUMP
-
mutant enzyme M190E, at 37C
0.0012
-
dUMP
Q8QTF3, -
at 30C
0.0021
-
dUMP
C6GJB8, -
at 30C
0.0023
-
dUMP
-
apparent value, wild type enzyme, pH not specified in the publication, at 37C
0.00259
-
dUMP
-
wild type enzyme, at 37C
0.004
-
dUMP
-, P67044
-
0.0044
-
dUMP
-
apparent value, mutant enzyme V3Y, pH not specified in the publication, at 37C
0.0054
-
dUMP
-
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 25C
0.0078
-
dUMP
-
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 25C
0.011
-
dUMP
-
apparent value, mutant enzyme V3T, pH not specified in the publication, at 37C
0.01563
-
dUMP
-
mutant enzyme L198P, at 37C
0.022
-
dUMP
-
apparent value, mutant enzyme V3A, pH not specified in the publication, at 37C
0.05
-
dUMP
-
10fold higher than wild-type thymidylate synthase; mutant K48Q
0.109
-
dUMP
-
apparent value, mutant enzyme V3L, pH not specified in the publication, at 37C
0.134
-
dUMP
-
apparent value, mutant enzyme V3F, pH not specified in the publication, at 37C
0.179
-
dUMP
-
mutant enzyme M190K, at 37C
0.065
-
L-5,10-methylenetetrahydrofolate
-
-
0.266
-
L-5,10-methylenetetrahydrofolate
-
-
0.0045
-
L-tetrahydrofolate
-
-
0.008
-
methylenetetrahydrofolate
-
-
0.008
-
methylenetetrahydrofolate
-
mutant Y4F
0.0081
-
methylenetetrahydrofolate
-
wild-type
0.0085
-
methylenetetrahydrofolate
-
wild-type
0.0097
-
methylenetetrahydrofolate
-
mutant S167A
0.01
-
methylenetetrahydrofolate
-
wild-type
0.01
-
methylenetetrahydrofolate
-
wild-type
0.011
-
methylenetetrahydrofolate
-
-
0.012
-
methylenetetrahydrofolate
-
mutant S167A
0.013
-
methylenetetrahydrofolate
-
mutant Y4H
0.015
-
methylenetetrahydrofolate
-
mutant Y4V
0.016
-
methylenetetrahydrofolate
-
-
0.018
-
methylenetetrahydrofolate
-
-
0.018
-
methylenetetrahydrofolate
-
mutant Y4I
0.0253
-
methylenetetrahydrofolate
-
-
0.027
-
methylenetetrahydrofolate
-
-
0.03
-
methylenetetrahydrofolate
-
native enzyme
0.031
-
methylenetetrahydrofolate
-
-
0.035
-
methylenetetrahydrofolate
-
-
0.037
-
methylenetetrahydrofolate
-
-
0.0382
-
methylenetetrahydrofolate
P45351
-
0.039
-
methylenetetrahydrofolate
-
recombinant enzyme
0.0426
-
methylenetetrahydrofolate
-
mutant S167G
0.0521
-
methylenetetrahydrofolate
-
mutant S167T
0.0627
-
methylenetetrahydrofolate
-
mutant S167T
0.092
-
methylenetetrahydrofolate
-
mutant TS N229C; mutant TS N229D
0.13
-
methylenetetrahydrofolate
-
mutant S167C
0.17
-
methylenetetrahydrofolate
-
mutant TS N229D, dCMP as substrate
0.3125
-
methylenetetrahydrofolate
-
-
0.001
-
methylenetetrahydropteroylgluamate
-
mutant P254S
0.0011
-
methylenetetrahydropteroylgluamate
-
wild-type
0.0012
-
methylenetetrahydropteroylgluamate
-
mutant P254G
0.0018
-
methylenetetrahydropteroylgluamate
-
mutant P254F
0.0118
-
methylenetetrahydropteroylgluamate
-
mutant P254D
0.0211
-
N5,N10-methylenetetrahydrofolate
-
-
0.077
-
tetrahydropteroylglutamate
-
-
0.0065
-
[6R]methylenetetrahydropteroyldiglutamate
-
-
0.0043
-
[6R]methylenetetrahydropteroylglutamate
-
-
0.0043
-
[6R]methylenetetrahydropteroylheptaglutamate
-
-
0.0087
-
[6R]methylenetetrahydropteroylhexaglutamate
-
-
0.0083
-
[6R]methylenetetrahydropteroylpentaglutamate
-
-
0.0109
-
[6R]methylenetetrahydropteroyltetraglutamate
-
-
0.0035
-
[6R]methylenetetrahydropteroyltriglutamate
-
-
TURNOVER NUMBER [1/s]
TURNOVER NUMBER MAXIMUM[1/s]
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.583
-
2'-Deoxyuridine
-
-
1.67
-
2'-Deoxyuridine
-
-
16
-
2'-Deoxyuridine
-
-
0.84
-
5,10-methylenetetrahydrofolate
P13922
D4 N-terminal tail mutant enzyme
1.2
-
5,10-methylenetetrahydrofolate
P13922
wild type enzyme
1.4
-
5,10-methylenetetrahydrofolate
P13922
Ala-FACE mutant enzyme with residues 284, 285, 288, 289, and 292 mutated to Ala
2.8
-
5,10-methylenetetrahydrofolate
Q8QTF3, -
at 30C
3.9
-
5,10-methylenetetrahydrofolate
-
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 25C
4.1
-
5,10-methylenetetrahydrofolate
C6GJB8, -
at 30C
48
-
5,10-methylenetetrahydrofolate
-
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 25C
0.4
-
deoxyuridine phosphate
-, P67044
22C
4.17
-
deoxyuridine phosphate
-
-
18
-
deoxyuridine phosphate
-, P67044
22C
0.016
-
dUMP
-
mutant K48Q
0.03
-
dUMP
-
mutant enzyme M190K, at 37C
0.52
-
dUMP
-
mutant enzyme A191K, at 37C
0.53
-
dUMP
-
mutant enzyme M190E, at 37C
1.64
-
dUMP
-
mutant enzyme L198P, at 37C
3.11
-
dUMP
-
wild type enzyme, at 37C
3.9
-
dUMP
-
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 25C
48
-
dUMP
-
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 25C
kcat/KM VALUE [1/mMs-1]
kcat/KM VALUE [1/mMs-1] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
70
-
5,10-methylenetetrahydrofolate
-
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 25C
4973
3200
-
5,10-methylenetetrahydrofolate
-
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 25C
4973
1.6e-07
-
dUMP
-
mutant enzyme M190K, at 37C
10224
0.0001
-
dUMP
-
mutant enzyme L198P, at 37C
10224
0.00055
-
dUMP
-
mutant enzyme M190E, at 37C
10224
0.00061
-
dUMP
-
mutant enzyme A191K, at 37C
10224
0.0012
-
dUMP
-
wild type enzyme, at 37C
10224
720
-
dUMP
-
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 25C
10224
6150
-
dUMP
-
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 25C
10224
Ki VALUE [mM]
Ki VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
1.8e-05
-
(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
-, P67044
22C
0.0027
-
1,3-propanediphosphonic acid
-
pH 7.2, 22C
0.016
-
1-(2'-deoxyribosyl)-8-azapurin-2-one 5'-monophosphate
-
-
0.12
-
1-(beta-D-2'-deoxyribofuranosyl)-1,6-dihydro-8-azapurin-2(3H,6H)-one 5'-monophosphate
-
-
0.022
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 recombinant enzyme
0.0321
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0049
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate
-
L1210 recombinant enzyme
0.0085
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0008
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0014
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate
-
L1210 recombinant enzyme
0.0013
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate
-
L1210 recombinant enzyme
0.00191
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0034
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 recombinant enzyme
0.00746
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0017
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 parental enzyme
0.0093
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate
-
L1210 recombinant enzyme
0.0075
-
10-formyldihydropteroylglutamate
-
-
0.0007
-
10-formyldihydropteroylheptaglutamate
-
-
-
0.0016
-
10-formyldihydropteroylpentaglutamate
-
-
0.0001
-
10-Formyltetrahydrofolylheptaglutamate
-
-
0.0024
-
10-Formyltetrahydrofolylmonoglutamate
-
-
0.02
-
10-formyltetrahydropteroylmonoglutamate
-
-
0.00477
-
2',5-difluoro-ara-UMP
-
-
0.4328
-
2'-deoxy-2',2'-difluorouridine 5'-dihydrogen
-
-
0.0103
-
2'-fluoro-ara-UMP
-
-
0.03
-
2,4-diamino pteridine
-
-
0.0013
-
2,4-diamino quinazoline
-
-
0.003
-
2,4-diamino quinazoline antifolate
-
-
0.01
-
5-bromo-2'-deoxyuridine 5'-monophosphate
-
-
0.0054
-
5-bromoacetamido-5'-deoxythymidine
-
competitive inhibition
0.0066
-
5-bromoacetamido-5'-deoxythymidine
-
-
2e-06
-
5-fluoro-2'-deoxyuridine 5'-monophosphate
-, P67044
22C; inhibited both ThyA and ThyX
1.4e-05
-
5-fluoro-2'-deoxyuridine 5'-monophosphate
-
-
0.0001
-
5-fluoro-2'-deoxyuridine 5'-monophosphate
-, P67044
22C
0.0011
-
5-fluoro-2'-deoxyuridine-5'-monophosphate
-
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 25C
0.0054
-
5-fluoro-2'-deoxyuridine-5'-monophosphate
-
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 25C
1e-06
-
5-fluoro-2'-deoxyuridylic acid
-
-
1.7e-06
-
5-fluoro-2'-deoxyuridylic acid
-
-
2e-06
-
5-fluoro-2'-deoxyuridylic acid
-
-
4e-06
-
5-fluoro-2'-deoxyuridylic acid
-
-
5e-06
-
5-fluoro-2'-deoxyuridylic acid
-
-
5e-06
-
5-fluoro-2'-deoxyuridylic acid
-
-
5e-06
-
5-fluoro-2'-deoxyuridylic acid
-
-
2e-05
-
5-fluoro-2'-deoxyuridylic acid
-
L1210 parental enzyme
2.1e-05
-
5-fluoro-2'-deoxyuridylic acid
-
50 nM
2.35e-05
-
5-fluoro-2'-deoxyuridylic acid
-
-
2.6e-05
-
5-fluoro-2'-deoxyuridylic acid
-
200 nM
5e-05
-
5-fluoro-2'-deoxyuridylic acid
-
-
0.002
-
5-fluoro-2'-deoxyuridylic acid
-
-
1e-05
-
5-Formyl-2'-deoxyuridylic acid
-
-
1.2e-05
-
5-Formyl-2'-deoxyuridylic acid
-
-
1.3e-05
-
5-Formyl-2'-deoxyuridylic acid
-
-
1e-05
-
5-Mercapto-2'-deoxyuridylic acid
-
-
4e-05
-
5-Mercapto-2'-deoxyuridylic acid
-
-
2.9e-05
-
5-Nitro-2'-deoxyuridine 5'-monophosphate
-
-
3.9e-05
-
5-trifluoromethyl-2'-deoxyuridine 5'-monophosphate
-
-
1e-05
-
5-trifluoromethyl-2'-deoxyuridylic acid
-
-
5
-
aminofolate
-
1.0 mM
5.2
-
aminofolate
-
5.0 mM
0.015
-
aminopterin
-
-
0.02
-
aminopterin
-
-
0.0347
-
aminopterin
-
-
0.0015
-
bromo-2'-deoxyuridine
-
L1210 parental enzyme
9e-05
-
CB3717
P13100
-
0.0003
-
chloro-2'-deoxyuridine
-
L1210 parental enzyme
4e-06
-
Cibacron blue
-
-
6e-08
-
D1694
-
-
2.8e-06
-
D1694
-
-
1e-06
-
D1694 pentaglutamate
-
-
1.5e-06
-
D1694 pentaglutamate
-
-
0.0075
-
deaza-aminopterin
-
-
0.0014
-
dihydrofolate
-
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
-
1.0 mM, noncompetitive inhibition, dUMP as variable substrate
0.0084
-
dithiophosphate
-
-
0.059
-
dTMP
-
-
0.07
-
dTMP
-
variable substrate 2'-deoxyuridine
0.14
-
dTMP
-
-
0.24
-
dTMP
-
variable substrate 5,10-methylenetetrahydropteroylglutamate
12
-
glyceraldehyde 3-phosphate
-
-
1.8e-05
-
GW1843U89
-, P67044
-
0.0037
-
hydroxymethyl-2'-deoxyuridine
-
L1210 parental enzyme
0.00768
-
iodo-2'-deoxyuridine
-
L1210 parental enzyme
0.0029
-
methasquin
-
-
0.023
-
methopterin
-
-
0.0284
-
methopterin
-
-
0.073
-
methopterin
-
variable substrate 2'-deoxyuridine
0.02
-
methotrexate
-
-
0.023
-
methotrexate
-
uncompetitive with methylene tetrahydrofolate
0.103
-
methotrexate
-
uncompetitive with dUMP
0.238
-
methotrexate
-
0.05 mM
0.267
-
methotrexate
-
0.02 mM
0.406
-
methotrexate
-
0.5 mM
0.413
-
methotrexate
-
1.0 mM
0.0001
-
Procion blue
-
variable substrate 2'-deoxyuridine
0.00022
-
Procion blue
-
variable substrate 5,10-methylenetetrahydropteroylglutamate
5.9e-06
-
propylene diphosphonate
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22C
-
1.13e-05
-
propylene diphosphonate
-
mutant enzyme A191K, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22C
-
0.0132
-
pteroyldiglutamate
-
-
0.0034
-
Pteroylheptaglutamate
-
-
0.002
-
pteroylhexaglutamate
-
-
0.0076
-
pteroylmonoglutamate
-
-
0.001
-
pteroylpentaglutamate
-
-
0.0006
-
pteroyltetraglutamate
-
-
0.0034
-
Pteroyltriglutamate
-
-
0.6
0.9
pyridoxal 5'-phosphate
-
-
0.0044
-
quinaspar
-
-
0.0013
-
SK 28,757
-
-
0.0015
-
SK 28,758
-
-
0.0029
-
SK 28,815
-
-
-
0.00012
-
tetrahydromethotrexate
-
-
0.0017
-
thiophosphate
-
-
0.001
-
thymidine phosphate
-
0.25 mM, noncompetitive inhibition, 5,10-mehylenetetrahydrofolate as variable substrate
0.00124
-
thymidine phosphate
-
1.0 mM, noncompetitive inhibition, 5,10-methylenetetrahydrofolate as variable substrate
0.0073
-
thymidine phosphate
-
L1210 parental enzyme
0.08
-
thymidine phosphate
-
-
0.12
-
thymidine phosphate
-
-
0.3125
-
thymidine phosphate
-
0.25 mM, competitive inhibition, dUMP as variable substrate
0.333
-
thymidine phosphate
-
-
0.000833
-
trimethoprim
-
1.0 mM
0.00087
-
trimethoprim
-
2.0 mM
0.852
-
trimethoprim
-
-
3.8e-05
-
ZD9331
-
pH 7.2, 22C
IC50 VALUE [mM]
IC50 VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
5.4e-05
-
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
-
-
0.00027
-
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
-
-
0.00015
-
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9 yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
C6GJB8, -
at 30C
0.00019
-
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9 yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
Q8QTF3, -
at 30C
1.9e-05
-
10-propargyl-5,8-dideazafolate
-
-
-
8.5e-05
-
10-propargyl-5,8-dideazafolate
-
-
-
0.00017
-
10-propargyl-5,8-dideazafolate
C6GJB8, -
at 30C
-
0.00023
-
10-propargyl-5,8-dideazafolate
Q8QTF3, -
at 30C
-
0.00043
-
10-propargyl-5,8-dideazafolate
-
-
-
0.0046
-
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.023
-
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
IC50 above 0.023 mM
0.0011
-
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.002
-
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0025
-
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00011
-
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0012
-
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0023
-
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00023
-
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.001
-
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0023
-
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00069
-
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
-
-
0.0012
-
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
-
-
0.0016
-
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
-
-
0.0012
-
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0018
-
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0023
-
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00038
-
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0018
-
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0023
-
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00039
-
2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0022
-
2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00075
-
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0022
-
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0025
-
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0011
-
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0014
-
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0023
-
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0056
-
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0084
-
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.028
-
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00028
-
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0017
-
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.002
-
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0013
-
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0026
-
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0029
-
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00022
-
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.001
-
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0017
-
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00012
-
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0012
-
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0024
-
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.00011
-
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
0.0012
-
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
-
5e-06
-
5-Fluoro-2-deoxyuridine
-
FM3A/0 cell
2.8e-06
-
5-fluoro-dUMP
-
FM3A/0 cell
0.00031
-
5-Fluorouracil
-
FM3A/0 cell
2.2e-08
-
FdUMP[10]
-
FdUMP[10] strongly inhibited cell growth in both FM3A cell lines, with a much lower resistance factor than FUdR and FdUMP
2.2e-05
-
FdUMP[10]
-
pH 7.4, 37C
0.000164
-
GW1843U89
-
FM3A/0 cell
0.018
-
methotrexate
-
at 30C and pH 7.4
0.029
-
methotrexate
-
at 30C and pH 7.4
0.09
-
methotrexate
-
at 30C and pH 7.4
4.6e-05
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
-
potent dual inhibitor of human TS and human DHFR, 2-fold more potent than PDDF and 206-fold more potent than pemetrexed
6.9e-05
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
-
potent inhibitor of human TS
0.00023
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
-
moderate inhibitor of human thymidylate synthase
4e-05
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydrothieno(2,3-d)pyrimidin-5-yl)sulfanyl)benzoyl)-L-glutamic acid
-
potent inhibitor of human TS and of human DHFR, it is a novel dual TS-DHFR inhibitor, 330-fold more potent than pemetrexed
5.4e-05
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
-
potent inhibitor of human TS and moderate inhibitor of human DHFR
0.00027
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
-
moderate inhibitor of human TS
0.047
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
-
-
0.0049
-
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
-
-
0.0054
-
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
at 30C and pH 7.4
0.027
-
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
at 30C and pH 7.4
0.23
-
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
at 30C and pH 7.4
1.8e-05
-
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
-
-
5.4e-05
-
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
-
-
9e-05
-
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
-
-
4.6e-05
-
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
-
-
6.9e-05
-
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
-
-
0.00023
-
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
-
-
3.6e-05
-
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
-
4e-05
-
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
-
0.0048
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
-
-
0.00128
-
nolatrexed
-
FM3A/0 cell
3.6e-05
-
pemetrexed
-
FM3A/0 cell
0.0028
-
pemetrexed
-
-
0.0028
-
pemetrexed
-
at 30C and pH 7.4
0.0095
-
pemetrexed
-
-
0.0095
-
pemetrexed
-
at 30C and pH 7.4
0.076
-
pemetrexed
-
-
0.076
-
pemetrexed
-
at 30C and pH 7.4
1.6e-05
-
raltitrexed
-
FM3A/0 cell
0.00038
-
raltitrexed
-
at 30C and pH 7.4
0.0009
-
raltitrexed
-
at 30C and pH 7.4
0.0057
-
raltitrexed
-
at 30C and pH 7.4
0.00144
-
ZD1694
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22C
0.034
-
ZD1694
-
mutant enzyme A191K, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22C
4e-05
-
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
-
additional information
-
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
value above 0.05
additional information
-
N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
value above 0.05
0.008
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
additional information
-
N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
value above 0.05
SPECIFIC ACTIVITY [µmol/min/mg]
SPECIFIC ACTIVITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
0.00012
-
-
-
0.00035
-
-
-
0.00035
-
-
intracellular form
0.00038
-
-
-
0.00119
-
-
blood form
0.00156
-
-
culture form
0.002135
-
-
Gardner lymphosarcoma
0.00235
-
-
-
0.003519
-
-
sarcoma 180
0.0063
-
-
-
0.01
-
-
-
0.0156
-
-
-
0.016
-
-
-
0.1024
-
-
-
0.6778
-
-
-
1.26
-
-
pH 7.2, 22C
1.3
-
-
affinity chromatography
1.33
-
-
-
3.8
-
-
50% pure preparation
210
-
-, P67044
22C, recombinant protein; 22C, recombinant protien
414
-
-
purified enzyme, in 50 mM Tris-HCl buffer (pH 8.0), at 37C
pH OPTIMUM
pH MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
5.9
-
-
UMP as substrate
6.5
6.8
-
phosphate buffer
6.6
6.8
-
-
6.6
-
-
-
6.7
-
-
-
7
8
-
activity is higher in Tris buffer than in phosphate buffer
7
8.1
-
-
7.2
7.4
-
double pH-optimum in 2-N-morpholinoethane sulfonic acid buffer
7.3
8
-
half-maximal activity at pH 6.3
7.5
-
-
-
pH RANGE
pH RANGE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
5.5
7.8
-
phosphate buffer
5.5
8
-
-
6
9
-
activity is negligible below pH 6.0 and above pH 9.0
6.2
9.5
-
Tris buffer
TEMPERATURE OPTIMUM
TEMPERATURE OPTIMUM MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
55
-
-
mutant enzyme, 2 disulfide bridges across the dimer interface of the enzyme engineered
TEMPERATURE RANGE
TEMPERATURE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
30
70
-
mutant enzyme, 2 disulfide bridges across the dimer interface of the enzyme engineered
SOURCE TISSUE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
SOURCE
-
from patients with acute myelocytic leukemia
Manually annotated by BRENDA team
-
intracellular parasites, host blood
Manually annotated by BRENDA team
-
intracellular parasites, host blood; obtained from infected rat blood
Manually annotated by BRENDA team
-
intracellular parasites, host blood
Manually annotated by BRENDA team
-
intracellular parasites, host blood; obtained from infected rat blood
Manually annotated by BRENDA team
-
colon cancer cell
Manually annotated by BRENDA team
-
adenocarcinoma
Manually annotated by BRENDA team
-
advanced colorectal cancer
Manually annotated by BRENDA team
Caenorhabditis elegans Bristol N2
-
-
-
Manually annotated by BRENDA team
-
; FM3A/TK- cell, mouse mammary carcinoma derived cell, deficient in thymidine kinase; FM3A/TSc cell, mouse mammary carcinoma derived cell, deficient in thymidylate synthase; mouse mammary carcinoma derived cell
Manually annotated by BRENDA team
-
normal human fibroblast cell line immortalized by SV40
Manually annotated by BRENDA team
-
parasitic helminth, obtained from the pulmonary hearts and vessels of infected Wistar albino rats
Manually annotated by BRENDA team
-
additionally transfected with pLGC-hUgi and pLGCX plasmids
Manually annotated by BRENDA team
-
; folate receptor-positive human epidermoid KB cell
Manually annotated by BRENDA team
-
highest thymidylate synthase expression
Manually annotated by BRENDA team
-
neonatal mouse liver
Manually annotated by BRENDA team
Rattus norvegicus Wistar
-
-
-
Manually annotated by BRENDA team
-
colorectal cancer cell, mutated subline of Lovo-92 cell
Manually annotated by BRENDA team
-
colorectal cancer cell, mutated subline of Lovo-92 cell
Manually annotated by BRENDA team
-
human colon carcinoma cell line
Manually annotated by BRENDA team
-
wildtype p53 colorectal cancer cell
Manually annotated by BRENDA team
-
colorectal cancer cell harboring a functionally inactive p53
Manually annotated by BRENDA team
-
human NSCLC cell line
Manually annotated by BRENDA team
-
human NSCLC cell line
Manually annotated by BRENDA team
-
human NSCLC cell line
Manually annotated by BRENDA team
-
human NSCLC cell line
Manually annotated by BRENDA team
-
human NSCLC cell line
Manually annotated by BRENDA team
-
L1210 leukemia cells grown in the peritoneal cavity of CDF1 mice
Manually annotated by BRENDA team
-
derived from primary malignant melanoma
Manually annotated by BRENDA team
-
thymus gland
Manually annotated by BRENDA team
-
; human colon carcinoma cell line
Manually annotated by BRENDA team
-
human NSCLC cell line
Manually annotated by BRENDA team
additional information
-
NCI60 panel of 60 human tumor cell lines, the NCI-60 model is able to provide interesting information about the role of TYMS gene polymorphisms on TYMS mRNA expression and catalytic activity
Manually annotated by BRENDA team
additional information
A6M9A2, -
expressed early after Geobacillus virus E2 infection
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
PDB
SCOP
CATH
ORGANISM
Bacillus subtilis (strain 168)
Bacillus subtilis (strain 168)
Bacillus subtilis (strain 168)
Bacillus subtilis (strain 168)
Bacillus subtilis (strain 168)
Brucella melitensis biotype 1 (strain 16M / ATCC 23456 / NCTC 10094)
Corynebacterium glutamicum (strain ATCC 13032 / DSM 20300 / JCM 1318 / LMG 3730 / NCIMB 10025)
Corynebacterium glutamicum (strain ATCC 13032 / DSM 20300 / JCM 1318 / LMG 3730 / NCIMB 10025)
Cryptococcus neoformans var. neoformans serotype D (strain JEC21 / ATCC MYA-565)
Encephalitozoon cuniculi (strain GB-M1)
Enterococcus faecalis (strain ATCC 700802 / V583)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Escherichia coli (strain K12)
Staphylococcus aureus (strain Mu50 / ATCC 700699)
MOLECULAR WEIGHT
MOLECULAR WEIGHT MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
31000
-
A6M9A2, -
recombinant GVE2-TS protein, SDS-PAGE
34000
38000
-
gel filtration, sucrose density-gradient centrifugation
35000
-
P45351
SDS-PAGE
35840
-
P45351
cDNA sequence
36620
-
-
calculated molecular mass based on the sequence
55000
-
-
gel filtration
57000
-
-, P67044
gel filtration; gel filtration
58000
-
-
-
58000
-
-
sucrose density gradient analysis
58000
-
B5U9U8, -
SDS-PAGE, bifunctional native BgDHFR-TS enzyme from the parasite lysate
58800
-
-
calculated from amino acid sequence
60000
-
-
-
63000
64000
-
gel filtration
64000
-
-
-
64400
-
-
sedimentation equilibrium measurement
65000
-
-
gel filtration, velocity sedimentation electrophoresis
66000
-
-
gel filtration
67000
-
-
Ehrlich ascites carcinoma cells, gel filtration
67000
-
-
Ehrlich ascites carcinoma cells, gel filtration
68000
-
-
gel filtration
69000
-
-
Ehrlich ascites carcinoma cells
70000
-
-
gel filtration
70000
-
-
-
70000
-
-
-
71000
-
-
Ehrlich ascites carcinoma cells, SDS-PAGE
71000
-
-
Ehrlich ascites carcinoma cells, SDS-PAGE
71000
-
-
analytical ultracentrifugation
72000
-
P04818
-
75000
-
-
L1210 cells, gel filtration
75000
-
-
dynamic light scattering
76000
-
-
-
76000
-
-
L1210 cells, purified enzyme, gel filtration
77000
-
-
gel filtration
78000
-
-
L1210 cells, gel filtration
100000
-
-
sedimentation in sucrose density gradients
104000
-
-, P67044
gel filtration
110000
-
-
-
132000
-
-
gel filtration
148000
-
-
presence of inhibitor 1,3-propanediphosphonic acid, dynamic light scattering
175000
-
-
gel filtration