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6.3.2.17: tetrahydrofolate synthase

This is an abbreviated version!
For detailed information about tetrahydrofolate synthase, go to the full flat file.

Word Map on EC 6.3.2.17

Reaction

ATP
+
tetrahydropteroyl-[gamma-Glu]n
+
L-glutamate
=
ADP
+
phosphate
+
tetrahydropteroyl-[gamma-Glu]n+1

Synonyms

100194131, AtDFB, cFPGS, DHFS/FPGS, dihydrofolate synthase/folylpolyglutamate synthase, eFPGS, Folate polyglutamate synthetase, FolC, folyl-gamma-glutamate synthetase, Folylpoly(.gamma.-glutamate) synthase, Folylpoly-.gamma.-glutamate synthase, Folylpoly-gamma-glutamate synthetase, Folylpoly-gamma-glutamate synthetase-dihydrofolate synthetase, Folylpolyglutamate synthase, Folylpolyglutamate synthetase, folylpolyglutamate synthetase 1, Folylpolyglutamyl synthetase, folypoly-gamma-glutamate synthetase, folypolyformyl glutamate synthase, folypolyglutamate synthase, folypolyglutamate synthetase, Formyltetrahydropteroyldiglutamate synthetase, FPGS, FPGS1, FPGS2, GRMZM2G393334, mFGPS, mFPGS, More, MTHFD1L, N10-Formyltetrahydropteroyldiglutamate synthetase, PfDHFS-FPGS, Synthetase, folylpolyglutamate, Tail length regulator, tetrahydrofolate:L-glutamate gamma-ligase (ADP-forming), tetrahydrofolylpolyglutamate synthase

ECTree

     6 Ligases
         6.3 Forming carbon-nitrogen bonds
             6.3.2 Acid—amino-acid ligases (peptide synthases)
                6.3.2.17 tetrahydrofolate synthase

IC50 Value

IC50 Value on EC 6.3.2.17 - tetrahydrofolate synthase

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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000008 - 13
(2S)-2-(o-fluoro-p-(N-(2,7-dimethyl-4-oxo-3,4-dihydroquinazolin-6-yl)methyl)-N-(prop-2-ynyl-amino)benzamido)-4-(tetrazol-5-yl)butyric acid
0.0000012
(S)-2(5-(((1,2-dihydro-3-methyl-1-oxobenzo-(f)quinazolin-9-yl)methyl)-1-oxo-2-isoindolinyl))-glutaric acid
Homo sapiens
-
IC50 of 0.0000009 mM in the wild type cell line, IC50 of 0.0000012 mM to 0.000539 mM in the antifolates-resistant sublines
0.00039
2-[[[(3S)-3-[(4-[[(2-amino-4-oxo-3,4-dihydropteridin-6-yl)methyl]amino]benzoyl)amino]-3-carboxypropyl](hydroxy)phosphoryl]methyl]pentanedioic acid
Plasmodium falciparum
-
-
0.000143 - 13
5,10-dideaza-5,6,7,8-tetrahydrofolic acid
0.0000095 - 0.0000175
methotrexate
0.000001 - 13
methotrexate-Glu
0.000008
methotrexate-phosphinate
Homo sapiens
-
competitive inhibition, IC50 of 0.000008 mM, at fixed substrate and recombinant enzyme concentrations. The most potent FPGS inhibitor based on methotrexate heterocycle. CCRF-CEM R2 subline does not respond to inhibition by this compound at 0.001 mM
0.00012
methotrexate-phosphonate
Homo sapiens
-
IC50 0.00012 mM, at fixed substrate and recombinant enzyme concentrations
0.000116 - 13
N-(4-(2(2-amino-3,4-dihydro-4-oxo-7H-pyrolo-(2,3-d)pyrimidine-5-yl)ethyl)-benzoyl)-L-glutamic acid
Mus musculus
-
IC50 of 0.0000136 mM in the wild type cell line, IC50 of 0.000116 mM in the MTA-13 cell line
0.000028 - 13
N-(5-(N-(3,4-dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N-methylamino)-2-thenoyl)L-glutamic acid
0.000006
Nalpha-(4-amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl-L-ornithine
Homo sapiens
-
IC50 of 0.000001 mM in the wild type cell line, IC50 of 0.000006 mM to 0.0017 mM in the antifolates-resistant sublines
0.000011 - 0.0000302
pemetrexed
additional information
2-[[[(4S)-4-carboxy-4-[(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)amino]butyl](hydroxy)phosphoryl]methyl]pentanedioic acid