Information on EC 2.1.2.2 - phosphoribosylglycinamide formyltransferase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY hide
2.1.2.2
-
RECOMMENDED NAME
GeneOntology No.
phosphoribosylglycinamide formyltransferase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide = tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
formyl group transfer
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
5-aminoimidazole ribonucleotide biosynthesis I
-
-
Biosynthesis of antibiotics
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-
Biosynthesis of secondary metabolites
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-
Metabolic pathways
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-
One carbon pool by folate
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-
Purine metabolism
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-
tetrahydrofolate salvage from 5,10-methenyltetrahydrofolate
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-
purine metabolism
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-
sulfopterin metabolism
-
-
tetrahydrofolate metabolism
-
-
SYSTEMATIC NAME
IUBMB Comments
10-formyltetrahydrofolate:5'-phosphoribosylglycinamide N-formyltransferase
-
CAS REGISTRY NUMBER
COMMENTARY hide
9032-02-4
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
fragment
SwissProt
Manually annotated by BRENDA team
pigeon
-
-
Manually annotated by BRENDA team
chinese hamster
-
-
Manually annotated by BRENDA team
strain TX635
-
-
Manually annotated by BRENDA team
rabbit
-
-
Manually annotated by BRENDA team
sheep
-
-
Manually annotated by BRENDA team
; strain PAO1
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-
Manually annotated by BRENDA team
rat
-
-
Manually annotated by BRENDA team
fission yeast
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-
Manually annotated by BRENDA team
pig
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
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)
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(6R)-N10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
(6R)-tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
show the reaction diagram
10-formyl-5,8-dideazafolate + beta-glycinamide ribonucleotide
5,8-dideazafolate + N-formyl beta-glycinamide ribonucleotide
show the reaction diagram
-
-
-
-
?
10-formyl-5,8-dideazafolate + carbocyclic beta-glycinamide ribonucleotide
5,8-dideazafolate + N-formyl carbocyclic beta-glycinamide ribonucleotide
show the reaction diagram
10-formyl-5,8-dideazafolate + N1-(5-phospho-D-ribosyl)glycinamide
?
show the reaction diagram
-
-
-
-
?
10-formyltetrahydrofolate + (alpha,beta)-glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
show the reaction diagram
-
-
-
?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
show the reaction diagram
10-formyltetrahydrofolate + beta-5-phospho-D-ribosylglycinamide
tetrahydrofolate + beta-5'-phosphoribosyl-N-formylglycinamide
show the reaction diagram
10-formyltetrahydrofolate + carbocyclic beta-glycinamide ribonucleotide
tetrahydrofolate + formyl glycinamide ribonucleotide
show the reaction diagram
10-formyltetrahydrofolate + glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
show the reaction diagram
10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide
tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
show the reaction diagram
10-formyltetrahydrofolate + N5-hydroxyornithine
tetrahydrofolate + N2-formyl-N5-hydroxyornithine
show the reaction diagram
-
-
-
-
?
10-formyltetrahydrofolate + N5-hydroxyornithine
tetrahydrofolate + N5-formyl-N5-hydroxyornithine
show the reaction diagram
-
-
-
-
?
10-formyltetrahydrofolate + O-phosphonate carbocyclic glycinamide ribonucleotide
tetrahydrofolate + O-phosphonate-ribosyl-N-formylglycinamide
show the reaction diagram
-
-
-
-
?
acetate + ATP
acetyl phosphate + ADP
show the reaction diagram
beta-glycinamide ribonucleotide + 10-formyltetrahydrofolate
?
show the reaction diagram
-
-
-
-
?
beta-glycinamide ribonucleotide + ATP + formate
beta-formylglycinamide ribonucleotide + ADP
show the reaction diagram
-
assay at 25°C
-
-
?
formate + ATP + beta-glycinamide ribonucleotide
beta-formylglycinamide ribonucleotide + ADP
show the reaction diagram
inosinic acid + glycinamide ribotide + H2O
5-amino-4-imidazolecarboxamide ribotide + formylglycinamide ribotide
show the reaction diagram
-
-
-
-
?
N10-formyl-5-deazafolate + glycinamide ribonucleotide
formylglycinamide ribonucleotide + 5-deazafolate
show the reaction diagram
-
-
-
-
?
N10-formyl-8-deazafolate + glycinamide ribonucleotide
formylglycinamide ribonucleotide + 8-deazafolate
show the reaction diagram
-
-
-
-
?
N10-formyldideazafolate + 5-phospho-D-ribosylglycinamide
dideazafolate + 5'-phosphoribosyl-N-formylglycinamide
show the reaction diagram
-
-
-
-
?
N10-formylfolate + glycinamide ribonucleotide
folate + formylglycinamide ribonucleotide
show the reaction diagram
-
-
-
-
?
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
show the reaction diagram
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-
-
-
ir
N5,N10-anhydroformyltetrahydrofolate + glycinamide ribotide + H2O
N10-formyltetrahydrofolate + formylglycinamide ribotide
show the reaction diagram
N5,N10-anhydroformyltetrahydrofolic acid + glycinamide ribonucleotide
formylglycinamide ribonucleotide + ?
show the reaction diagram
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-
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-
?
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
show the reaction diagram
10-formyltetrahydrofolate + glycinamide ribonucleotide
tetrahydrofolate + formylglycinamide ribonucleotide
show the reaction diagram
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
10-formyl-5,8-dideazafolate
10-formyltetrahydrofolate
-
binding structure and formyl transfer structure and mechanism analysis, overview
5,10-methenyltetrahydrofolate
-
-
folate
formate
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second GAR transformylase using formate and ATP in place of 10-formyltetrahydrofolate
L-(+-)-5,10-methenyltetrahydrofolate
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-
L-(-)-10-formyltetrahydrofolate
N10-formyltetrahydrofolate
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Fe2+
-
expression regulated by amount of iron in the growth medium
K+
-
activity enhanced by
lometrexol
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-
Mg2+
-
purT gene product
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2S)-2-(((5-(2-((6R)-2-amino-4-oxo-5,6,7,8-tetrahydro-1 H-pyrido[2,3-d]-pyrimidin-6-yl)ethyl)thiophene-2-yl)carbonyl)amino)-pentanedioic acid
-
LY309887
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(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
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AG2034
-
(2S)-2-[[4-[(1RS)-1-[(2, 4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid
-
-
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(6R)-5,10-dideazatetrahydrofolate
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lometrexol
(6R)-dideazatetrahydrofolate diglutamate
(6R)-dideazatetrahydrofolate pentaglutamate
(6R)-dideazatetrahydrofolate tetraglutamate
(6R)-dideazatetrahydrofolate triglutamate
(6S)-dideazatetrahydrofolate
(6S)-N10-formyltetrahydrofolate
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-
(alpha,beta)-hydroxyacetamide ribonucleotide
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-
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
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-
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
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(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
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(S)-2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)pentanedioic acid
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(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
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(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
-
-
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(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
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(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
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lometrexol, LMTX
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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
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-
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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
10-Acetyl-5,8-dideazafolate
10-CF3CO-DDACTHF
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-
10-formyl-5,10-dideaza-5,6,7,8-tetrahydrofolic acid
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10-formyl-5,8-dideazafolic acid hexaglutamate
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10-formyl-DDACTHF
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10-methanesulfonyl-5-DACTHF
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10-methanesulfonyl-DDACTHF
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10-methylthio-DDACTHF
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10-trifluoroacetyl-DDACTHF
2',3'-dideoxy-2',3'-didehydro-carbocyclic glycinamide ribonucleotide
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2',3'-dideoxy-carbocyclic glycinamide ribonucleotide
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2',5'-furan-dideazatetrahydrofolate
2',5'-thiophene dideazatetrahydrofolate
2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-N-[[(pyridin-3-ylmethyl)-carbamoyl]-methyl]-acetamide
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-
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2-deaminodideazatetrahydrofolate
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3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-propionamide
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-
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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
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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
-
-
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4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-benzamide
-
-
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4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-butyramide
-
-
-
5'-phosphonate carbocyclic glycinamide ribonucleotide
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-
5,10-dideaza-5,6,7,8-tetrahydrofolate
5,10-dideaza-5,6,7,8-tetrahydrofolic acid
-
-
5,10-dideazafolic acid
-
-
5,10-dideazatetrahydrofolate
5,8-Dideazafolate
-
-
5,8-dideazafolate hexaglutamate
-
-
5,8-dideazapteroyl hexaglutamate
-
-
5-deazatetrahydrofolate
-
-
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
-
-
-
AG2034
-
-
AG2037
-
-
alpha,beta-hydroxyacetamideribonucleotide
-
-
alpha,beta-N-(hydroxyacetyl)-D-ribofuranosylamine
-
-
beta-thioglycinamide dideazafolate
-
-
DDACTHF
dideazafolate
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-
dideazatetrahydrofolate
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dideazatetrahydrofolate hexaglutamate
-
-
homo-dideazatetrahydrofolate
-
-
L-(+)-10-formyltetrahydrofolate
-
excellent competitive inhibitor
lometrexol
LY231514
-
antitumor activity may result from simultaneous and multiple inhibition of several key folate-requiring enzymes via its polyglutamated metabolites
LY231514 monoglutamate
-
-
LY231514 pentaglutamate
-
-
LY309887
-
-
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-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic 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
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-
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
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-
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
-
-
N10-(Bromoacetyl)-5,8-dideazafolate
-
-
N10-formyl-2,4-diaminodideazafolate
-
-
pemetrexed
permetrexed
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
glycine
-
stimulatory effect
histidine
-
stimulatory effect
NH4+
-
activity enhanced by
tryptophan
-
stimulatory effect
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0775 - 0.0848
(6R)-N10-formyltetrahydrofolate
0.000075 - 33
10-formyl-5,8-dideazafolate
0.019
5,8-Dideazafolate
-
-
0.00368
acetate
-
purT gene product
0.0774
ATP
-
purT gene product
0.0011 - 33
beta-glycinamide ribonucleotide
0.0036 - 0.0465
carbocyclic beta-glycinamide ribonucleotide
-
0.018
carbocyclic glycinamide ribonucleotide
-
-
0.319
formate
-
purT gene product
0.102
formyl-beta-glycinamide ribonucleotide
-
-
-
0.01 - 0.4
glycinamide ribonucleotide
0.052
glycinamide ribotide
-
-
0.00576
L-(+)-5,10-methenyltetrahydrofolate
-
-
0.0008 - 0.00676
L-(-)-10-formyltetrahydrofolate
0.21
N-formylglycinamide ribotide
-
-
0.0211 - 0.099
N10-formyl-5,8-dideazafolate
0.19
N10-formyl-5-deazafolate
-
-
0.15
N10-Formyl-8-deazafolate
-
-
0.0167 - 0.0365
N10-formyldideazafolate
0.6
N10-formylfolate
-
-
0.058
N5,N10-anhydroformyl tetrahydrofolate
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
13.5 - 20.7
(6R)-N10-formyltetrahydrofolate
0.0019 - 0.102
10-formyl-5,8-dideazafolate
0.0034 - 14
beta-glycinamide ribonucleotide
33
carbocyclic glycinamide ribonucleotide
Escherichia coli
-
-
16.1 - 40
N10-formyl-5,8-dideazafolate
1.52
N10-formyl-5-deazafolate
Escherichia coli
-
-
0.069
N10-Formyl-8-deazafolate
Escherichia coli
-
-
0.016
N10-formylfolate
Escherichia coli
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
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
-
-
0.000015 - 0.00003
10-CF3CO-DDACTHF
0.000014
10-formyl-DDACTHF
0.00058
10-methanesulfonyl-5-DACTHF
-
26°C, pH 7.5
0.00023
10-methanesulfonyl-DDACTHF
-
26°C, pH 7.5
0.00025
10-methylthio-DDACTHF
0.000015 - 0.0019
10-trifluoroacetyl-DDACTHF
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
0.0017 - 0.005
DDACTHF
0.0093
LY231514 monoglutamate
-
-
0.000065
LY231514 pentaglutamate
-
-
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, 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
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
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
0.000016 - 0.01
10-CF3CO-DDACTHF
0.0027 - 0.1
DDACTHF
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
0.00003 - 0.02
pemetrexed
additional information
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.651
-
-
0.95
-
-
1.294
-
-
14
-
purN gene product
additional information
-
purT gene product, 0.052 mg /min.mg.mL
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5
-
in vitro GARFT enzyme inhibition assay
7.8
-
Tris buffer, 38°C
8.5 - 8.8
-
-
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5 - 11
-
-
6 - 9.5
-
-
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
xenograft HXGC3, HC1 and VRC5
Manually annotated by BRENDA team
-
the enzyme is frequently overexpressed in glioma, enzyme immunohistochemic analysis in 70 cases of human gliomas and normal brain tissues, overview
Manually annotated by BRENDA team
-
O cell
Manually annotated by BRENDA team
-
enzyme expression and functional significance in hepatocellular carcinoma cells from several patients, overview
Manually annotated by BRENDA team
-
murine leukemia
Manually annotated by BRENDA team
-
murine lymphoma cell line
Manually annotated by BRENDA team
-
xenograft, pancreatic carcinoma
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
PDB
SCOP
CATH
ORGANISM
UNIPROT
Anaplasma phagocytophilum (strain HZ)
Aquifex aeolicus (strain VF5)
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)
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)
Geobacillus kaustophilus (strain HTA426)
Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
11200
-
1 * 12100 + 1 * 11200, heterodimer, SDS-PAGE
12100
-
1 * 12100 + 1 * 11200, heterodimer, SDS-PAGE
21060
-
calculated from peptide sequence deduced from the cDNA
21700
x * 21700, calculated, x * 26000, SDS-PAGE of recombinant protein including His-tag
21800
-
recombinant enzyme, predicted from cDNA
21840
-
recombinant enzyme, MALDI-TOF mass spectral analysis
24000
-
equilibrium sedimentation ultracentrifugation
25700
-
SDS-PAGE
26000
x * 21700, calculated, x * 26000, SDS-PAGE of recombinant protein including His-tag
30985
-
x * 30985, calculated
31000
-
DNA sequencing
41900
-
product of the purT gene, SDS-PAGE
42000
-
product of the purT gene, deduced from predicted amino acid sequence
42400
-
product of the purT gene
55000
-
2 * 55000, SDS-PAGE, sucrose density ultracentrifugation, proteolytic cleavage
63000
-
2 * 63000, transformylase, homodimer, SDS-PAGE
70000
-
gel filtration
83000
-
2 * 83000, trifunctional protein, SDS-PAGE
95000
-
2 * 95000, trifunctional protein, SDS-PAGE
100000
102000
-
1 * 102000, SDS-PAGE
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
112000
-
HeLa and L1210 cells
115000
-
-
117000
-
ultracentrifugation
125000
-
sucrose density gradient ultracentrifugation
140000
-
sucrose density ultracentrifugation
150000
160000
-
trifunctional protein, sucrose density gradient ultracentrifugation
190000
-
trifunctional protein, sucrose density gradient ultracentrifugation
201000
218000
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
diffraction to 2.5 A, space group P3121
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
-
orthorhombic space group C222, a = 141.4 A, b = 98.2 A, c = 103.5 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
-
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 10
-
-
485741
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-10°C, 8months, no appreciable loss of activity
-
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
-
partially
-
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 enzyme, expressed in E. coli
-
recombinant His-tagged enzyme from Escherichia coli strain BL21 (DE3) by nickel affinity and anion exchange chromatography, and gel filtration
-
recombinant protein
transformylase, product of the purT gene
-
using a NiHisTrap HP column, the affinity tag is removed by cleavage with TEV protease
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
; pvdF gene characterization
-
cDNA, recombinant enzyme expressed in insect cells with a recombinant baculovirus
-
cloned and expressed in Escherichia coli BL21(DE3)pLysS
-
cloned and expressed in Escherichia coli HMS174(DE3)/pCC12
-
cloned by functional complementation in Escherichia coli
-
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
-
enzyme expression analysis in hepatocellular carcinoma cell lines, overview
-
expression in Escherichia coli
gene purN, recombinant expression of C-terminally His-tagged enzyme in Escherichia coli strain BL21(DE3)
-
harboring expression vector pJS167, encoding the purN gene
-
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
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D144E
-
catalytically inactive mutant
D144H
-
catalytically inactive mutant
H108K
-
catalytically inactive mutant
H108R
-
catalytically inactive mutant
K170R
-
catalytically active mutant
N106D
-
catalytically inactive mutant
N106H
-
catalytically inactive mutant
N106Q
-
catalytically active mutant
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
diagnostics
medicine
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