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Information on EC 2.1.2.2 - phosphoribosylglycinamide formyltransferase
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2.1.2.2 phosphoribosylglycinamide formyltransferaseSpecify your search results
Word Map
- 2.1.2.2
- purine
-
antifolate
- thymidylate
- dihydrofolate
- pemetrexed
-
formylation
-
folic
-
polyglutamation
-
folate-dependent
-
aminoimidazole
-
ccrf-cem
-
multitargeted
-
folylpolyglutamate
-
trifunctional
-
5,10-dideazatetrahydrofolic
-
alimta
- medicine
- aicar
-
ddathf
- lometrexol
- mta
-
pyrrolo2,3-dpyrimidine
-
folate-requiring
-
phosphoribosylaminoimidazole
- trimetrexate
- monoglutamate
- raltitrexed
-
aminoimidazolecarboxamide
- 5-aminoimidazole-4-carboxamide
-
6-substituted
- 5-formyltetrahydrofolate
-
antipurine
-
igrov1
- diagnostics
-
formylglycinamide
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
Reaction Schemes
Synonyms
glycinamide ribonucleotide formyltransferase, glycinamide ribonucleotide transformylase, garft, gar tfase, gar transformylase, garftase, glycinamide ribonucleotide formyl transferase, gar formyltransferase, 
more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
2-amino-N-ribosylacetamide 5'-phosphate (glycinamide ribotide) transformylase
-
-
2-amino-N-ribosylacetamide 5'-phosphate transformylase
-
-
-
-
5,10-methenyltetrahydrofolate:2-amino-N-ribosylacetamide ribonucleotide transformylase
-
-
-
-
GAR formyltransferase
GAR TFase
GAR transformylase
-
-
-
-
GARFT
GARFTase
GART
GART synthetase
glycinamide ribonucleotide formyltransferase
glycinamide ribonucleotide transformylase
N10-formyltetrahydrolate:2-amino-N-ribosylacetamide-5'-phosphate transformylase
GAR formyltransferase
-
-
-
-
GAR TFase
-
-
-
-
glycinamide ribonucleotide transformylase
-
-
-
-
N10-formyltetrahydrolate:2-amino-N-ribosylacetamide-5'-phosphate transformylase
-
-
N10-formyltetrahydrolate:2-amino-N-ribosylacetamide-5'-phosphate transformylase
Escherichia coli B / ATCC 11303
-
-
-
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide = tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
-
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
formyl group transfer
formyl group transfer
-
-
-
-
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PATHWAY SOURCE
PATHWAYS
KEGG
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SYSTEMATIC NAME
IUBMB Comments
10-formyltetrahydrofolate:5'-phosphoribosylglycinamide N-formyltransferase
-
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CAS REGISTRY NUMBER
COMMENTARY
9032-02-4
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(6R)-N10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
(6R)-tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
10-formyl-5,8-dideazafolate + beta-glycinamide ribonucleotide
5,8-dideazafolate + N-formyl beta-glycinamide ribonucleotide
-
-
-
-
?
10-formyl-5,8-dideazafolate + carbocyclic beta-glycinamide ribonucleotide
5,8-dideazafolate + N-formyl carbocyclic beta-glycinamide ribonucleotide
10-formyltetrahydrofolate + (alpha,beta)-glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
10-formyltetrahydrofolate + beta-5-phospho-D-ribosylglycinamide
tetrahydrofolate + beta-5'-phosphoribosyl-N-formylglycinamide
10-formyltetrahydrofolate + carbocyclic beta-glycinamide ribonucleotide
tetrahydrofolate + formyl glycinamide ribonucleotide
10-formyltetrahydrofolate + glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide
tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
10-formyltetrahydrofolate + N5-hydroxyornithine
tetrahydrofolate + N2-formyl-N5-hydroxyornithine
-
-
-
-
?
10-formyltetrahydrofolate + N5-hydroxyornithine
tetrahydrofolate + N5-formyl-N5-hydroxyornithine
-
-
-
-
?
10-formyltetrahydrofolate + O-phosphonate carbocyclic glycinamide ribonucleotide
tetrahydrofolate + O-phosphonate-ribosyl-N-formylglycinamide
-
-
-
-
?
beta-glycinamide ribonucleotide + ATP + formate
beta-formylglycinamide ribonucleotide + ADP
-
assay at 25°C
-
-
?
formate + ATP + beta-glycinamide ribonucleotide
beta-formylglycinamide ribonucleotide + ADP
inosinic acid + glycinamide ribotide + H2O
5-amino-4-imidazolecarboxamide ribotide + formylglycinamide ribotide
-
-
-
-
?
N10-formyl-5-deazafolate + glycinamide ribonucleotide
formylglycinamide ribonucleotide + 5-deazafolate
-
-
-
-
?
N10-formyl-8-deazafolate + glycinamide ribonucleotide
formylglycinamide ribonucleotide + 8-deazafolate
-
-
-
-
?
N10-formyldideazafolate + 5-phospho-D-ribosylglycinamide
dideazafolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
N10-formylfolate + glycinamide ribonucleotide
folate + formylglycinamide ribonucleotide
-
-
-
-
?
N5,N10-anhydroformyl-5,6,7,8tetrahydrofolic acid + 2-amino-N-ribosylacetamide 5'-phosphate + H2O
formylglycinamide ribotide + tetrahydrofolic acid + 2-formamido-N-ribosylacetamide 5'-phosphate
-
-
-
-
ir
N5,N10-anhydroformyltetrahydrofolate + glycinamide ribotide + H2O
N10-formyltetrahydrofolate + formylglycinamide ribotide
N5,N10-anhydroformyltetrahydrofolic acid + glycinamide ribonucleotide
formylglycinamide ribonucleotide + ?
-
-
-
-
?
(6R)-N10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
(6R)-tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
(6R)-N10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
(6R)-tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
(6R)-N10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
(6R)-tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyl-5,8-dideazafolate + carbocyclic beta-glycinamide ribonucleotide
5,8-dideazafolate + N-formyl carbocyclic beta-glycinamide ribonucleotide
-
-
-
?
10-formyl-5,8-dideazafolate + carbocyclic beta-glycinamide ribonucleotide
5,8-dideazafolate + N-formyl carbocyclic beta-glycinamide ribonucleotide
-
-
-
-
?
10-formyl-5,8-dideazafolate + carbocyclic beta-glycinamide ribonucleotide
5,8-dideazafolate + N-formyl carbocyclic beta-glycinamide ribonucleotide
-
-
-
-
?
10-formyl-5,8-dideazafolate + carbocyclic beta-glycinamide ribonucleotide
5,8-dideazafolate + N-formyl carbocyclic beta-glycinamide ribonucleotide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
485714, 485715, 485718, 485719, 485720, 485727, 485728, 485729, 485730, 485731, 485732, 485733, 485734, 485735, 485736, 485738, 485740, 485741
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
r
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
third step in de novo purine biosynthetic pathway
-
-
r
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
Escherichia coli B / ATCC 11303
-
-
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
in uricotelic organisms such as birds, the major role of this active pathway is elimination of waste nitrogen
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
transformylation reaction of purine biosynthesis
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
in ureotelic animals such as mammals the role of the far less active pathway is to provide purine nucleotides for further anabolic sequences
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
third step in de novo purine biosynthetic pathway
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
carries out the second, third and fifth sequential reactions of de novo purine synthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
involved in pyoverdine synthesis
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + beta-5-phospho-D-ribosylglycinamide
tetrahydrofolate + beta-5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
-
10-formyltetrahydrofolate + beta-5-phospho-D-ribosylglycinamide
tetrahydrofolate + beta-5'-phosphoribosyl-N-formylglycinamide
-
-
-
?
10-formyltetrahydrofolate + beta-5-phospho-D-ribosylglycinamide
tetrahydrofolate + beta-5'-phosphoribosyl-N-formylglycinamide
Escherichia coli B / ATCC 11303
-
-
-
-
-
10-formyltetrahydrofolate + carbocyclic beta-glycinamide ribonucleotide
tetrahydrofolate + formyl glycinamide ribonucleotide
-
-
-
-
?
10-formyltetrahydrofolate + carbocyclic beta-glycinamide ribonucleotide
tetrahydrofolate + formyl glycinamide ribonucleotide
-
-
-
-
?
10-formyltetrahydrofolate + carbocyclic beta-glycinamide ribonucleotide
tetrahydrofolate + formyl glycinamide ribonucleotide
-
-
-
-
?
10-formyltetrahydrofolate + glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
-
-
-
-
?
10-formyltetrahydrofolate + glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
-
-
-
-
?
10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide
tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
-
-
-
-
?
10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide
tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
-
-
-
-
?
acetate + ATP
acetyl phosphate + ADP
-
novel non-folate glycinamide ribonucleotide transformylase purT gene product, no significant homology to known EC 2.1.2.2 but significant homology to the purK protein also involved in purine biosynthesis
-
-
?
acetate + ATP
acetyl phosphate + ADP
-
novel non-folate glycinamide ribonucleotide transformylase purT gene product, no significant homology to known EC 2.1.2.2 but significant homology to the purK protein also involved in purine biosynthesis
-
-
?
formate + ATP + beta-glycinamide ribonucleotide
beta-formylglycinamide ribonucleotide + ADP
-
novel non-folate glycinamide ribonucleotide transformylase purT gene product, no significant homology to known EC2.1.2.2 but significant homology to the purK protein also involved in purine biosynthesis
-
-
?
formate + ATP + beta-glycinamide ribonucleotide
beta-formylglycinamide ribonucleotide + ADP
-
novel non-folate glycinamide ribonucleotide transformylase purT gene product, no significant homology to known EC2.1.2.2 but significant homology to the purK protein also involved in purine biosynthesis
-
-
?
N5,N10-anhydroformyltetrahydrofolate + glycinamide ribotide + H2O
N10-formyltetrahydrofolate + formylglycinamide ribotide
-
-
-
-
?
N5,N10-anhydroformyltetrahydrofolate + glycinamide ribotide + H2O
N10-formyltetrahydrofolate + formylglycinamide ribotide
-
-
-
-
-
additional information
?
-
-
10-formyl-dideazaformate, 5-formyltetrahydroformate, formylaminoimidazolecarboxamide ribonucleotide, formylmethionine, formiminoglutamate, GTP, CTP, TTP, ITP and ZTP are no substrates for the purT GAR transformylase
-
-
-
additional information
?
-
-
purT GAR transformylase is the first unknown de novo purine biosynthetic enzyme to be discovered in the last 30 years and represents another step forward in understanding cellular control of purine levels
-
-
-
additional information
?
-
-
10-formyl-dideazaformate, 5-formyltetrahydroformate, formylaminoimidazolecarboxamide ribonucleotide, formylmethionine, formiminoglutamate, GTP, CTP, TTP, ITP and ZTP are no substrates for the purT GAR transformylase
-
-
-
additional information
?
-
-
purT GAR transformylase is the first unknown de novo purine biosynthetic enzyme to be discovered in the last 30 years and represents another step forward in understanding cellular control of purine levels
-
-
-
additional information
?
-
-
reaction does not occur if glycine, glycinamide or glycinamide riboside is substituted for glycinamide ribotide
-
-
-
additional information
?
-
-
glycinamide ribonucleotide nucleoside is no substrate
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
GAR transformylase activity copurifies with 5,10-methylene-, 5,10-methenyl, and 10-formyl-H4folate sythetase (combined) trifunctional enzyme, EC 6.3.4.3, EC 1.5.1.5 and EC 3.5.4.9
-
-
-
additional information
?
-
-
purified along with 10-formyltetrahydrofolate synthetase
-
-
-
additional information
?
-
-
uses both diastereomers of 5,10-methenyltetrahydrofolate, (+)-L-diastereomer is used 120 times faster than the (-)-L-diastereomer
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
alpha-glycinamide ribonucleotide and glycinamide ribonucleotide nucleoside are neither substrates for no inhibitors
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
additional information
?
-
-
trifunctional enzyme, GAR synthetase, aminoimidazole ribonucleotide synthetase and GAR transformylase
-
-
-
additional information
?
-
-
3 activities in a multifunctional protein, posessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotidetransformylase and aminoimidazole ribonucleotide synthetase
-
-
-
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
10-formyltetrahydrofolate + glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
third step in de novo purine biosynthetic pathway
-
-
r
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
in uricotelic organisms such as birds, the major role of this active pathway is elimination of waste nitrogen
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
transformylation reaction of purine biosynthesis
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
in ureotelic animals such as mammals the role of the far less active pathway is to provide purine nucleotides for further anabolic sequences
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
third step in de novo purine biosynthetic pathway
-
-
-
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
essential enzyme in DNA synthesis, third enzyme in de novo purine biosynthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
carries out the second, third and fifth sequential reactions of de novo purine synthesis pathway
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
involved in pyoverdine synthesis
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
-
-
-
?
10-formyltetrahydrofolate + glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
-
-
-
-
?
10-formyltetrahydrofolate + glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
-
-
-
-
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
10-formyltetrahydrofolate
-
binding structure and formyl transfer structure and mechanism analysis, overview
formate
-
second GAR transformylase using formate and ATP in place of 10-formyltetrahydrofolate
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2S)-2-(((5-(2-((6R)-2-amino-4-oxo-5,6,7,8-tetrahydro-1H-pyrido[2,3-d]-pyrimidin-6-yl)ethyl)thiophene-2-yl)carbonyl)amino)-pentanedioic acid
-
LY309887
(2S)-2-(((5-(2-((6S)-2-amino-4-oxo-1,6,7,8-tetrahydropyrimido[5,4-b]-[1,4]thiazin-6-yl)ethyl)thiophene-2-yl)carbonyl)amino)-pentanedioic acid
-
AG2034
(2S)-2-[[4-[(1RS)-1-[(2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid
-
-
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
-
-
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
-
-
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
-
-
(S)-2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)pentanedioic acid
-
-
(S)-2-(4-(2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanedioic acid
-
-
(S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
-
-
(S)-2-(4-(3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)propyl)benzamido)pentanedioic acid
-
-
(S)-2-(4-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)butyl)benzamido)pentanedioic acid
-
-
(S)-2-(4-(5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)pentyl)benzamido)pentanedioic acid
-
-
(S)-2-(4-(6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)hexyl)benzamido)pentanedioic acid
-
-
(S)-2-(5-(3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)propyl)thiophene-2-carboxamido)pentanedioic acid
-
-
(S)-2-(5-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)butyl)thiophene-2-carboxamido)pentanedioic acid
-
-
(S)-2-(5-(5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)pentyl)thiophene-2-carboxamido)pentanedioic acid
-
-
(S)-2-(5-(6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)hexyl)thiophene-2-carboxamido)pentanedioic acid
-
lometrexol, LMTX
1-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetyl]-piperidine-4-carboxylic acid (pyridin-3-ylmethyl)-amide
-
-
10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid
-
specifically inhibits recombinant GAR Tfase, inactive against other folate-dependent enzymes, potent inhibitor of tumor cell proliferation
2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-N-[[(pyridin-3-ylmethyl)-carbamoyl]-methyl]-acetamide
-
-
3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-propionamide
-
-
4-([2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-methyl)-N-pyridin-3-ylmethyl-benzamide
-
inhibition of thymidylate synthase, as well as glycinamide ribonucleotide formyltransferase and ribonucleotide formyltransferase. Growth inhibition of 4-([2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-methyl)-N-pyridin-3-ylmethyl-benzamide toward KB cells results in cytotoxicity and G1/G2-phase accumulation, and is partially protected by excess thymidine and adenosine, but is completely reversed in the combination of thymidine and adenosine
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-cyclohexanecarboxylic acid (pyridin-3-ylmethyl)-amide
-
-
4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-benzamide
-
-
4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-butyramide
-
-
5-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-pentanoic acid (pyridin-3-ylmethyl)-amide
-
-
6-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-hexanoic acid (pyridin-3-ylmethyl)-amide
-
-
LY231514
-
antitumor activity may result from simultaneous and multiple inhibition of several key folate-requiring enzymes via its polyglutamated metabolites
N-(4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl)-L-glutamic acid
-
-
N-(4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-propyl]benzoyl)-L-glutamic acid
N-(4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-butyl]benzoyl)-L-glutamic acid
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
N-(4-[6-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-hexyl]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-(5-[N-(3,4-dihydro-2-methyl-4-oxyquinazolin-6-ylmethyl)-N-methyl-amino]-2-thienoyl)-L-glutamic acid
-
-
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
-
-
N-([5-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophen-2-yl]carbonyl)-L-glutamic acid
-
-
N-([5-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophen-2-yl]carbonyl)-L-glutamic acid
-
-
N-[(5-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]-4-methylthiophen-2-yl)carbonyl]glutamic acid
-
modeling
N-[(5-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]thiophen-2-yl)carbonyl]glutamic acid
-
modeling
N-[(5-[2-[(6S)-2-amino-4-oxo-4,6,7,8-tetrahydro-3H-pyrimido[5,4-b][1,4]thiazin-6-yl]ethyl]thiophen-2-yl)carbonyl]glutamic acid
-
modeling
N-[4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
-
binding structure analysis, modeling, overview
N-[4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
-
binding structure analysis, modeling, overview
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
-
-
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
N-[4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
-
-
N-[4-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
-
-
N-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
-
-
N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
-
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid
-
effective inhibitor
N-[4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]-L-glutamic acid
-
-
N-[4-[6-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1,1,1-trifluoro-2-oxohexan-3-yl]benzoyl]glutamic acid
-
-
N-[4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]-L-glutamic acid
-
-
N-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexanoyl]-L-glutamic acid
-
-
N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-L-glutamic acid
-
-
N-{4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic acid
-
-
N-{4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl}-L-glutamic acid
-
-
N-{4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl}-L-glutamic acid
-
-
2',5'-thiophene dideazatetrahydrofolate
-
LY309886, diastereomer A; LY309887, diastereomer B
2',5'-thiophene dideazatetrahydrofolate
-
LY309886, diastereomer A; LY309887, diastereomer B
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
-
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
-
4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
-
4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
-
N-(4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-propyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-propyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase
N-(4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-butyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-butyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase
N-(4-[6-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-hexyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[6-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-hexyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
-
-
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
-
-
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
-
-
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
-
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
-
additional information
-
10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF and 10-methylthio-DDACTHF shows KI-values above 0.1 mM
-
additional information
-
no inhibition by N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid
-
additional information
-
inhibitor design and evalutaion of cofactor analogues, C10 substitution and stereochemistry, pteridine-binding pocket structure and ligand binding, modeling, overview
-
additional information
-
synthesis and antitumor activity of a series of 6-substituted pyrrolo[2,3-d]pyrimidines as potential nonclassical antifolates targeting both thymidylate and purine nucleotide biosynthesis, docking study and molecular modeling using the enzyme's crystal structure in complex with compound 10-CF3CO-DDACTHF, PDB ID 1NJS. Growth inhibition of human cancer cells by the inhibitors, IC50 values, overview
-
additional information
-
synthesis of 5-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors that acts as a dual inhibitor of GARFTase and AICARFTase, EC 2.1.2.3, principal mechanism of action, overview. 8, with a 4-carbon bridge, is the most active analog and potently inhibits proliferation of folate receptor alpha-expressing Chinese hamster ovary and KB human tumor cells. Molecular modeling and docking studies, overview
-
additional information
-
design and synthesis of series of 6-substituted straight side chain pyrrolo[2,3-d]pyrimidines with varying chain lengths (n = 5-8), non-benzoyl 6-carbon chain pyrrolo[2,3-d]pyrimidine antifolates are inhibitors of cell proliferation, correlating with expression of folate receptors. The compounds show selective cellular uptake via folate receptor-alpha and -beta, associated with high affinity binding and inhibition of de novo purine nucleotide biosynthesis via the enzyme, resulting in potent inhibition against folate receptor-expressing Chinese hamster cells and human KB tumor cells in culture
-
additional information
-
design and synthesis of a series of 5-substituted thiopheneyl pyrrolo[2,3-d]pyrimidines with varying chain lengths (n = 1-6). The compounds show dual inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase, analysis of the unique structure-activity relationship for transport and dual target inhibition, molecular modeling and computational studies using crystal structure of human GARFTase at 1.60 A resolution, PDB ID 4EW2, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Adenocarcinoma
Derivation and characterization of a monoclonal antibody against human glycinamide ribonucleotide formyltransferase.
Adenocarcinoma
Efficient experimental design and nonparametric modeling of drug interaction.
Adenocarcinoma
Improved synthetic routes to 5,8-dideazapteroylglutamates amenable to the formation of poly-gamma-L-glutamyl derivatives.
Amyotrophic Lateral Sclerosis
The glycinamide ribonucleotide transformylase (GART) gene is not responsible for familial amyotrophic lateral sclerosis.
Anemia, Megaloblastic
Role of folate dependent transformylases in synthesis of purine in bone marrow of man and in bone marrow and liver of rats.
Arthritis, Experimental
Inhibition of glycinamide ribonucleotide formyltransferase results in selective inhibition of macrophage cytokine secretion in vitro and in vivo efficacy in rat adjuvant arthritis.
Arthritis, Experimental
LY309887, antifolate via the folate receptor suppresses murine type II collagen-induced arthritis.
Arthritis, Rheumatoid
Inhibition of glycinamide ribonucleotide formyltransferase results in selective inhibition of macrophage cytokine secretion in vitro and in vivo efficacy in rat adjuvant arthritis.
Arthritis, Rheumatoid
Metabolism-blocked antifolates as potential anti-rheumatoid arthritis agents: 4-amino-4-deoxy-5,8,10-trideazapteroyl-d,l-4'-methyleneglutamic acid (CH-1504) and its analogs.
Carcinoma
A defect in the p53 response pathway induced by de novo purine synthesis inhibition.
Carcinoma
Derivation and characterization of a monoclonal antibody against human glycinamide ribonucleotide formyltransferase.
Carcinoma
Effect of purine synthesis inhibition on WiDr spheroids in vitro or on WiDr or colon 38 tumors in vivo. Complete growth inhibition but not regression.
Carcinoma
MTA (LY231514) in combination treatment regimens using human tumor xenografts and the EMT-6 murine mammary carcinoma.
Carcinoma
TS, DHFR and GARFT expression in non-squamous cell carcinoma of NSCLC and malignant pleural mesothelioma patients treated with pemetrexed.
Carcinoma, Hepatocellular
Biochemical studies on PT523, a potent nonpolyglutamatable antifolate, in cultured cells.
Carcinoma, Hepatocellular
Increased expression of glycinamide ribonucleotide transformylase is associated with a poor prognosis in hepatocellular carcinoma, and it promotes liver cancer cell proliferation.
Carcinoma, Hepatocellular
Isolation and characterization of cDNA clones for rat liver 10-formyltetrahydrofolate dehydrogenase.
Carcinoma, Non-Small-Cell Lung
Association between expression of thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase and efficacy of pemetrexed in advanced non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
Derivation and characterization of a monoclonal antibody against human glycinamide ribonucleotide formyltransferase.
Glioma
Glycinamide ribonucleotide formyl transferase is frequently overexpressed in glioma and critically regulates the proliferation of glioma cells.
Head and Neck Neoplasms
Pemetrexed disodium in recurrent locally advanced or metastatic squamous cell carcinoma of the head and neck.
Infection
Novel nonclassical inhibitors of glycinamide ribonucleotide formyltransferase: 10-formyl and 10-hydroxymethyl derivatives of 5,8,10-trideazapteroic acid.
Leukemia
Biochemical and biological studies on 2-desamino-2-methylaminopterin, an antifolate the polyglutamates of which are more potent than the monoglutamate against three key enzymes of folate metabolism.
Leukemia
Biological and structural evaluation of 10R- and 10S-methylthio-DDACTHF reveals a new role for sulfur in inhibition of glycinamide ribonucleotide transformylase.
Leukemia
Cellular pharmacology of MTA: a correlation of MTA-induced cellular toxicity and in vitro enzyme inhibition with its effect on intracellular folate and nucleoside triphosphate pools in CCRF-CEM cells.
Leukemia
Evidence for a relationship between intracellular GTP levels and the induction of HL-60 leukemia cell differentiation by 5,10-dideazatetrahydrofolic acid (DDATHF).
Leukemia
Folate analogues. 31. Synthesis of the reduced derivatives of 11-deazahomofolic acid, 10-methyl-11-deazahomofolic acid, and their evaluation as inhibitors of glycinamide ribonucleotide formyltransferase.
Leukemia
Induction of HL-60 leukemia cell differentiation by tetrahydrofolate inhibitors of de novo purine nucleotide biosynthesis.
Leukemia
Inhibition of glycinamide ribonucleotide formyltransferase and other folate enzymes by homofolate polyglutamates in human lymphoma and murine leukemia cell extracts.
Leukemia
Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis.
Leukemia, Lymphoid
Cell cycle effects of antifolate antimetabolites: implications for cytotoxicity and cytostasis.
Liver Neoplasms
Increased expression of glycinamide ribonucleotide transformylase is associated with a poor prognosis in hepatocellular carcinoma, and it promotes liver cancer cell proliferation.
Lung Neoplasms
Association between expression of thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase and efficacy of pemetrexed in advanced non-small cell lung cancer.
Lymphoma
5,10-Methylenetetrahydro-5-deazafolic acid and analogues: synthesis and biological activities.
Lymphoma
Inhibition of glycinamide ribonucleotide formyltransferase and other folate enzymes by homofolate polyglutamates in human lymphoma and murine leukemia cell extracts.
Lymphoma
Mammalian glycinamide ribonucleotide transformylase: purification and some properties.
Lymphoma
Synthesis of 10-acetyl-5,8-dideazafolic acid: a potent inhibitor of glycinamide ribonucleotide transformylase.
Mesothelioma
TS, DHFR and GARFT expression in non-squamous cell carcinoma of NSCLC and malignant pleural mesothelioma patients treated with pemetrexed.
Neoplasms
5,10-Methenyltetrahydrofolate synthetase activity is increased in tumors and modifies the efficacy of antipurine LY309887.
Neoplasms
A novel class of monoglutamated antifolates exhibits tight-binding inhibition of human glycinamide ribonucleotide formyltransferase and potent activity against solid tumors.
Neoplasms
Biochemistry and pharmacology of glycinamide ribonucleotide formyltransferase inhibitors: LY309887 and lometrexol.
Neoplasms
Determinants of the disparate antitumor activities of (6R)-5,10-dideaza-5,6,7,8-tetrahydrofolate and methotrexate toward human lymphoblastic leukemia cells, characterized by severely impaired antifolate membrane transport.
Neoplasms
Effect of purine synthesis inhibition on WiDr spheroids in vitro or on WiDr or colon 38 tumors in vivo. Complete growth inhibition but not regression.
Neoplasms
Enhancement of antineoplastic activity of 5-fluorouracil in mice bearing colon 38 tumor by (6R)5,10-dideazatetrahydrofolic acid.
Neoplasms
Folic acid-enhanced synergy for the combination of trimetrexate plus the glycinamide ribonucleotide formyltransferase inhibitor 4-[2-(2-amino-4-oxo-4,6,7,8-tetrahydro-3H-pyrimidino[5,4,6][1,4]thiazin -6-yl)-(S)-ethyl]-2,5-thienoylamino-L-glutamic acid (AG2034): comparison across sensitive and resistant human tumor cell lines.
Neoplasms
Human glycinamide ribonucleotide transformylase: active site mutants as mechanistic probes.
Neoplasms
Loss of reduced folate carrier function and folate depletion result in enhanced pemetrexed inhibition of purine synthesis.
Neoplasms
MTA (LY231514) in combination treatment regimens using human tumor xenografts and the EMT-6 murine mammary carcinoma.
Neoplasms
Pemetrexed: mRNA expression of the target genes TS, GARFT and DHFR correlates with the in vitro chemosensitivity of human solid tumors.
Neoplasms
Phase I dose-escalation and pharmacokinetic study of a novel folate analogue AG2034.
Neoplasms
Phase I study of (6R)-5,10-dideazatetrahydrofolate: a folate antimetabolite inhibitory to de novo purine synthesis.
Neoplasms
Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid.
Neoplasms
Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors ? and ? and the proton-coupled folate transporter.
Neoplasms
Synergy between 5,10-dideaza-5,6,7,8-tetrahydrofolic acid and methotrexate in mice bearing L1210 tumors.
Neoplasms
Synthesis and biological activity of open-chain analogues of 5,6,7,8-tetrahydrofolic acid--potential antitumor agents.
Neoplasms
The role of dietary folate in modulation of folate receptor expression, folylpolyglutamate synthetase activity and the efficacy and toxicity of lometrexol.
Neoplasms
TS, DHFR and GARFT expression in non-squamous cell carcinoma of NSCLC and malignant pleural mesothelioma patients treated with pemetrexed.
Neoplasms
Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor ? and inhibition of de novo purine nucleotide biosynthesis.
Neoplasms
Whole-body disposition and polyglutamate distribution of the GAR formyltransferase inhibitors LY309887 and lometrexol in mice: effect of low-folate diet.
Neuroblastoma
5,10-Methenyltetrahydrofolate synthetase activity is increased in tumors and modifies the efficacy of antipurine LY309887.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Novel pyrrolo[2,3-d]pyrimidine antifolate TNP-351: cytotoxic effect on methotrexate-resistant CCRF-CEM cells and inhibition of transformylases of de novo purine biosynthesis.
Tuberculosis
Structures of Glycinamide Ribonucleotide Transformylase (PurN) from Mycobacterium tuberculosis Reveal a Novel Dimer with Relevance to Drug Discovery.
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.99
10-formyl-5,8-dideazafolate
-
chimeric enzyme GPG-N11 (hGART1-56/PurN57-131/hGART132-202)
4
10-formyl-5,8-dideazafolate
-
chimeric enzyme GPX-M1 (hGART1-100/PurN101-212); wild-type enzyme
33
10-formyl-5,8-dideazafolate
-
chimeric enzyme PGX-B12 (PurN1-101/hGART102-202)
0.008
beta-glycinamide ribonucleotide
-
pH 8.5, tetrahydrofolate as cofactor
0.012
beta-glycinamide ribonucleotide
-
pH 7.5, tetrahydrofolate as cofactor
0.0122
beta-glycinamide ribonucleotide
-
pH 7.5, tetrahydrofolate as cofactor
0.99
beta-glycinamide ribonucleotide
-
chimeric enzyme GPG-N11 (hGART1-56/PurN57-131/hGART132-202)
4
beta-glycinamide ribonucleotide
-
chimeric enzyme GPX-M1 (hGART1-100/PurN101-212); wild-type enzyme
12
beta-glycinamide ribonucleotide
-
chimeric enzyme GPX-M55 (hGART1-56/PurN58-212)
21
beta-glycinamide ribonucleotide
-
chimeric enzyme GPX-M24 (hGART1-54/PurN55-212)
33
beta-glycinamide ribonucleotide
-
chimeric enzyme PGX-B12 (PurN1-101/hGART102-202)
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0019
10-formyl-5,8-dideazafolate
-
chimeric enzyme GPX-M1 (hGART1-100/PurN101-212)
0.018
10-formyl-5,8-dideazafolate
-
chimeric enzyme GPX-M24 (hGART1-54/PurN55-212)
0.031
10-formyl-5,8-dideazafolate
-
chimeric enzyme GPX-M55 (hGART1-56/PurN58-212)
0.043
10-formyl-5,8-dideazafolate
-
chimeric enzyme GPG-N11 (hGART1-56/PurN57-131/hGART132-202)
0.102
10-formyl-5,8-dideazafolate
-
chimeric enzyme PGX-B12 (PurN1-101/hGART102-202)
0.0262
beta-glycinamide ribonucleotide
-
chimeric enzyme PGX-B12 (PurN1-101/hGART102-202)
0.0662
beta-glycinamide ribonucleotide
-
chimeric enzyme GPX-M1 (hGART1-100/PurN101-212)
0.262
beta-glycinamide ribonucleotide
-
chimeric enzyme GPX-M24 (hGART1-54/PurN55-212)
0.293
beta-glycinamide ribonucleotide
-
chimeric enzyme GPG-N11 (hGART1-56/PurN57-131/hGART132-202)
0.63
beta-glycinamide ribonucleotide
-
chimeric enzyme GPX-M55 (hGART1-56/PurN58-212)
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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00021
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
-
-
0.0014
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
-
-
0.0012
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
-
-
0.0011
(S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
-
-
0.000015
10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid
-
-
0.000056
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
26°C, pH 7.5
0.0048
4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
26°C, pH 7.5
0.0011
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
-
-
0.00085
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
-
-
0.00018
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
-
-
0.000005 - 0.00005
N-[(5-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]-4-methylthiophen-2-yl)carbonyl]glutamic acid
-
pH and temperature not specified in the publication
0.000005 - 0.00005
N-[(5-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]thiophen-2-yl)carbonyl]glutamic acid
-
pH and temperature not specified in the publication
0.000005 - 0.00005
N-[(5-[2-[(6S)-2-amino-4-oxo-4,6,7,8-tetrahydro-3H-pyrimido[5,4-b][1,4]thiazin-6-yl]ethyl]thiophen-2-yl)carbonyl]glutamic acid
-
pH and temperature not specified in the publication
0.00021
N-[4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
-
pH and temperature not specified in the publication
0.00018
N-[4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
-
pH and temperature not specified in the publication
0.00006
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
-
-
0.0005
N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid
-
26°C, pH 7.5
additional information
additional information
-
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid and 4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid show Ki-values above 0.1 mM
-
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00007 - 0.01
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
0.0005 - 0.01
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
0.0007 - 0.01
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
0.01 - 0.1
(S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
0.00852
N-(4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-propyl]benzoyl)-L-glutamic acid
Mus musculus
-
pH 7.5, 37°C
0.00551
N-(4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-butyl]benzoyl)-L-glutamic acid
Mus musculus
-
pH 7.5, 37°C
0.0024 - 0.01
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
0.0005 - 0.01
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
0.00005 - 0.01
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
0.001 - 0.02
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
0.000018 - 0.00244
N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
0.000014 - 0.1
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
0.0000068 - 0.00015
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
0.0000072 - 0.00226
N-[4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]-L-glutamic acid
0.0000086 - 0.00251
N-[4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]-L-glutamic acid
additional information
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
0.00007
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine
0.00008
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine
0.00009
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.0055
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.01
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine
0.0005
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.0006
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine
0.01
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.0007
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.0008
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.0009
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine
0.01
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.01
(S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine
0.1
(S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.000016
10-CF3CO-DDACTHF
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.000017
10-CF3CO-DDACTHF
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine
0.00006
10-CF3CO-DDACTHF
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.01
10-CF3CO-DDACTHF
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.0027
DDACTHF
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.0036
DDACTHF
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine
0.01
DDACTHF
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.1
DDACTHF
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine
0.0024
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.0044
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine
0.0055
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.0057
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine
0.01
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.0005
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.0006
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine
0.0007
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine
0.006
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.01
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine
0.00005
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.00006
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine
0.00007
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine
0.005
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.01
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine
0.001
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in situ
0.02
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
Mus musculus
-
in vitro
0.000018
N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
Homo sapiens
-
in situ
0.00244
N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
Mus musculus
-
in vitro
0.000014
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
Homo sapiens
-
in situ
0.0002
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine
0.00078
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
Mus musculus
-
in vitro
0.01
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
Homo sapiens
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine; in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine
0.1
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
Homo sapiens
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine
0.0000068
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
Homo sapiens
-
in situ
0.00015
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
Mus musculus
-
in vitro
0.0000072
N-[4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]-L-glutamic acid
Homo sapiens
-
in situ
0.00226
N-[4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]-L-glutamic acid
Mus musculus
-
in vitro
0.0000086
N-[4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]-L-glutamic acid
Homo sapiens
-
in situ
0.00251
N-[4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]-L-glutamic acid
Mus musculus
-
in vitro
additional information
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
Mus musculus
-
IC50 value above 0.02 mM, pH 7.5, 37°C
additional information
N-(4-[6-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-hexyl]benzoyl)-L-glutamic acid
Mus musculus
-
IC50 value above 0.02 mM, pH 7.5, 37°C
additional information
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
Homo sapiens
-
value above 0.05
additional information
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
additional information
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
additional information
N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
additional information
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
additional information
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
additional information
N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
chicken
1312, 172166, 485712, 485713, 485714, 485716, 485718, 485721, 485724, 485725, 485727, 485728, 485729, 485731, 485734, 485735, 485738, 485742
-
-
brenda
yeast
-
-
brenda
-
485714, 485715, 485718, 485719, 485720, 485727, 485728, 485730, 485731, 485732, 485734, 485735, 485736, 485738, 485739, 485740, 485741, 672526, 672527, 672528
-
-
brenda
enzymes displays phosphoribosylamine-glycine ligase activity, phosphoribosylformylglycinamidine cyclo-ligase activity and phosphoribosylglycinamide formyltransferase activity, cf. EC 6.3.4.13
Uniprot
brenda
human
-
-
brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
the enzyme is frequently overexpressed in glioma, enzyme immunohistochemic analysis in 70 cases of human gliomas and normal brain tissues, overview
brenda
-
enzyme expression and functional significance in hepatocellular carcinoma cells from several patients, overview
brenda
-
enzyme immunohistochemic analysis in 70 cases of human gliomas and normal brain tissues, overview
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
metabolism
-
glycinamide ribonucleotide transformylase is a folate-dependent enzyme in the de novo purine pathway
physiological function
additional information
-
the enzyme comprises residues 808-1010 for the hGAR Tfase domain (purN) from the native human trifunctional enzyme (purD-purM-purN)
malfunction
-
depletion of the enzyme by small interfering RNA inhibits cell proliferation and blocks S-phase and mitotic entry in cultured Hep-G2 and BEL-7404 cells. Enzyme depletion decreases the proliferating cell nuclear antigen concentration
malfunction
-
transfecting cells with GART-siRNA suppresses proliferation and enhances temozolomide-induced apoptosis in glioma cells
physiological function
-
increased expression of glycinamide ribonucleotide transformylase promotes liver cancer cell proliferation, enzyme expression and functional significance in hepatocellular carcinoma cells from several patients, overview
physiological function
-
glycinamide ribonucleotide formyl transferase is frequently overexpressed in glioma and critically regulates the proliferation of glioma cells
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PDB
SCOP
CATH
UNIPROT
ORGANISM
Q8YGB8
Brucella melitensis biotype 1 (strain 16M / ATCC 23456 / NCTC 10094)
Campylobacter jejuni subsp. jejuni serotype O:2 (strain ATCC 700819 / NCTC 11168)
Coxiella burnetii (strain RSA 493 / Nine Mile phase I)
Escherichia coli (strain K12)
Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
21700
x * 21700, calculated, x * 26000, SDS-PAGE of recombinant protein including His-tag
23000
23240
26000
x * 21700, calculated, x * 26000, SDS-PAGE of recombinant protein including His-tag
42000
-
product of the purT gene, deduced from predicted amino acid sequence
55000
-
2 * 55000, SDS-PAGE, sucrose density ultracentrifugation, proteolytic cleavage
61000
100000
108000
-
human GART comprises the C-terminal domain of a 108 kDa, trifunctional enzyme
110000 - 120000
-
gel filtration, sucrose density gradient ultracentrifugation, sedimentation velocity
110000
150000
201000
218000
100000
-
protein possessing transformylase activity, sucrose density gradient ultracentrifugation
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
dimer
monomer
?
x * 21700, calculated, x * 26000, SDS-PAGE of recombinant protein including His-tag
dimer
-
pH-dependent dimer-monomer transition near physiological pH might act as a means of regulating enzyme activity
dimer
-
2 * 61000, GAR transformylase, SDS-PAGE; 2 * 95000, trifunctional protein, SDS-PAGE
dimer
-
2 * 63000, transformylase, homodimer, SDS-PAGE; 2 * 83000, trifunctional protein, SDS-PAGE; homodimer
dimer
-
2 * 55000, SDS-PAGE, sucrose density ultracentrifugation, proteolytic cleavage; homodimer
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CRYSTALLIZATION/commentary
ORGANISM
UNIPROT
LITERATURE
crystals grown at 20°C by hanging-drop vapor diffusion, space group C222, a = 140.9 A, b = 97.6 A, c = 102.4
-
crystals grown by vapor diffusion, space group C222, a = 140.5 A, b = 98.2 A, c = 103.3 A
-
purified recombinant enzyme in apoform or in complex with inhibitors 10S methylthio-DDACTHF and 10R methylthio-DDACTHF, mixing of 0.002 ml of 15 mg/mL in 20 mM Tris, pH 8.0, 200 mM NaCl, 5 mM DTT, and inhibitors in a 5fold molar excess for complex crystals, with 0.002 ml of reservoir solution containing 0.1 M phosphate/citrate buffer, 1.5-2.0 M ammonium sulfate at pH 4.2, X-ray diffraction structure determination and analysis at 1.52-1.70 A resolution, molecular replacement
-
vapor diffusion sitting drop method, crystals of enzyme in complex with 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid
-
in complex with magnesium and iodide at 2.2 A resolution, and with cofactor analogue 5-methyltetrahydrofolate at 2.2 A resolution
purified recombinant enzyme, hanging drop vapour diffusion method, mixing of 0.001 ml of 22 mg/ml protein solution with 0.001 ml of reservoir solution containing 0.2 M lithium chloride, 0.1 M sodium cacodylate trihydrate, pH 6.6, 14% PEG 3350, and equilibration against 0.2 ml of reservoir solution, 18°C, method optimization, X-ray diffraction structure determination and analysis at 2.1 A resolution, molecular replacement
-
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
hybrid enzymes of human GART and PurN from Escherichia coli are expressed in Escherichia coli: PGX-B12 (PurN1-101/hGART102-202),GPX-M1 (hGART1-100/PurN101-212), GPX-M1 (hGART1129/PurN54-212), GPX-M24 (hGART1-54/PurN55-212), GPX-M36 (hGART1-89/PurN90-212), GPX-M55 (hGART1-56/PurN58-212), GPG-N11 (hGART1-56/PurN57-131/hGART132-202)
additional information
-
enzyme disruption mutant, no synthesis of pyoverdine, mutant strain is unable to grow on King´s B agar containing iron-chelating agent EDTA
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pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
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PURIFICATION/commentary
ORGANISM
UNIPROT
LITERATURE
copurification of trifunctional 5,10-methenyl-, 5,10-methylene, and 10-formylH4folate synthetase, aminoimidazole carboxamide ribotide transformylase and serine transhydroxymethylase
-
purified in combination with formyl-methenyl-methylenetetrahydrofolate synthetase
-
recombinant C-terminally His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and gel filtration
-
recombinant His-tagged enzyme from Escherichia coli strain BL21 (DE3) by nickel affinity and anion exchange chromatography, and gel filtration
-
using a NiHisTrap HP column, the affinity tag is removed by cleavage with TEV protease
-
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CLONED/commentary
ORGANISM
UNIPROT
LITERATURE
cDNA, recombinant enzyme expressed in insect cells with a recombinant baculovirus
-
cloning of a 12-gene cluster encoding 9 enzymes for de novo purine nucleotide synthesis
-
cloning, chromosomal assignment, genomic organization and the complete sequence of the bovine GART gene; cloning, chromosomal assignment, genomic organization and the complete sequence of the bovine GART gene; cloning, chromosomal assignment, genomic organization and the complete sequence of the bovine GART gene
coding region of Escherichia coli GART amplified from chromosomal DNA with PCR method
-
expression in Escherichia coli
gene purN, recombinant expression of C-terminally His-tagged enzyme in Escherichia coli strain BL21(DE3)
-
hybrid enzymes of human GART and PurN from Escherichia coli are expressed in Escherichia coli: PGX-B12 (PurN1-101/hGART102-202), GPX-M1 (hGART1-100/PurN101-212), GPX-M1 (hGART1129/PurN54-212), GPX-M24 (hGART1-54/PurN55-212), GPX-M36 (hGART1-89/PurN90-212), GPX-M55 (hGART1-56/PurN58-212), GPG-N11 (hGART1-56/PurN57-131/hGART132-202)
-
hybrid glycinamide ribonucleotide transformylase, ribonucleotide binding domain from purN, catalytic machinery and formyl tetrahydrofolate binding domain from purU encoded formyl tetrahydrofolate hydrolase
-
into the pET17b vector and into the pMC8HdeltaT vector for expression in Escherichia coli BL21Star(DE3)pRARE cells
-
recombinant expression of His-tagged enzyme in Escherichia coli strain BL21 (DE3)
-
second GAR transformylase encoded by the Escherichia coli purT gene
-
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
diagnostics
medicine
diagnostics
-
increased expression of glycinamide ribonucleotide transformylase is associated with a poor prognosis in hepatocellular carcinoma
diagnostics
-
GART expression is associated with glioma grade and high GART protein expression might be related to poor outcome
medicine
-
pharmacological importance, target enzyme for chemotherapy, development of novel antifolate drugs, to be used as anti-cancer drugs; target for structure-based drug design
medicine
-
pharmacological importance, target enzyme for chemotherapy, development of novel antifolate drugs, to be used as anti-cancer drugs
medicine
-
inhibitor 5,10-dideazatetrahydrofolate is antiproliferate and cytotoxic against mammalian tumor cells in culture and have broad spectrum activity against transplantable mouse tumors and human tumor xenografts
medicine
-
pharmacological importance, target enzyme for chemotherapy, development of novel antifolate drugs, to be used as anti-cancer drugs
medicine
-
pharmacological importance, target enzyme for chemotherapy, development of novel antifolate drugs, to be used as anti-cancer drugs
medicine
-
glycinamide ribonucleotide transformylase is a validated target for cancer chemotherapy
medicine
-
glycinamide ribonucleotide transformylase has emerged as a productive target for antineoplastic therapeutic intervention