Cloned (Comment) | Organism |
---|---|
gene purN, recombinant expression of C-terminally His-tagged enzyme in Escherichia coli strain BL21(DE3) | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
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 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
10-formyl-5,10-dideaza-5,6,7,8-tetrahydrofolic acid | - |
Homo sapiens | |
lometrexol | i.e. (6R)-5,10-dideaza-5,6,7,8-tetrahydrofolic acid | Homo sapiens | |
additional information | inhibitor design and evalutaion of cofactor analogues, C10 substitution and stereochemistry, pteridine-binding pocket structure and ligand binding, modeling, overview | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
N-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid | - |
Homo sapiens | |
N-[4-[6-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1,1,1-trifluoro-2-oxohexan-3-yl]benzoyl]glutamic acid | - |
Homo sapiens | |
permetrexed | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P22102 | - |
- |
Purification (Comment) | Organism |
---|---|
recombinant C-terminally His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and gel filtration | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
leukemia cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide | - |
Homo sapiens | tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide | - |
? |
Synonyms | Comment | Organism |
---|---|---|
GAR TFase | - |
Homo sapiens |
glycinamide ribonucleotide transformylase | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
10-formyltetrahydrofolate | binding structure and formyl transfer structure and mechanism analysis, overview | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens | |
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 | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
additional information | the enzyme comprises residues 808-1010 for the hGAR Tfase domain (purN) from the native human trifunctional enzyme (purD-purM-purN) | Homo sapiens |