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Literature summary extracted from

  • Deis, S.M.; Doshi, A.; Hou, Z.; Matherly, L.H.; Gangjee, A.; Dann, C.E.
    Structural and enzymatic analysis of tumor-targeted antifolates that inhibit glycinamide ribonucleotide formyltransferase (2016), Biochemistry, 55, 4574-4582 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.1.2.2 expressed in Escherichia coli Rosetta (DE3)pLysS cells Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.1.2.2 sitting drop vapor diffusion method, using 0.1 M Tris-HCl (pH 7.5), 0.333 M NaCl, 18% (w/v) polyethylene glycol (PEG) 4000, and a 2% (w/v) PEG 400 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.2.2 N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
 Homo sapiens
2.1.2.2 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
2.1.2.2 N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
-
 Homo sapiens
2.1.2.2 N-[5-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]-L-glutamic acid
-
 Homo sapiens
2.1.2.2 N-[5-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
-
 Homo sapiens
2.1.2.2 N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-D-glutamic acid
-
 Homo sapiens
2.1.2.2 N-[8-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)octanoyl]-D-glutamic acid
-
 Homo sapiens
2.1.2.2 pemetrexed
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.2.2 10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide Homo sapiens
-
 tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.2.2 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.1.2.2 Ni-NTA resin column chromatography and Superdex 75 gel filtration Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.2.2 10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide
-
 Homo sapiens tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.1.2.2 GARFTase
-
 Homo sapiens
2.1.2.2 glycinamide ribonucleotide formyltransferase
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.2.2 0.000007
-
 N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid at pH 7.5 and 37°C Homo sapiens
2.1.2.2 0.000009
-
 N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid at pH 7.5 and 37°C Homo sapiens
2.1.2.2 0.000017
-
 N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid at pH 7.5 and 37°C Homo sapiens
2.1.2.2 0.000022
-
 N-[5-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid at pH 7.5 and 37°C Homo sapiens
2.1.2.2 0.000067
-
 N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-D-glutamic acid at pH 7.5 and 37°C Homo sapiens
2.1.2.2 0.000068
-
 N-[5-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]-L-glutamic acid at pH 7.5 and 37°C Homo sapiens
2.1.2.2 0.000099
-
 N-[8-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)octanoyl]-D-glutamic acid at pH 7.5 and 37°C Homo sapiens
2.1.2.2 0.001067
-
 N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid at pH 7.5 and 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.1.2.2 0.00000017
-
 at pH 7.5 and 37°C Homo sapiens N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
2.1.2.2 0.00000026
-
 at pH 7.5 and 37°C Homo sapiens N-[5-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]-L-glutamic acid
2.1.2.2 0.00000027
-
 at pH 7.5 and 37°C Homo sapiens N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
2.1.2.2 0.00000055
-
 at pH 7.5 and 37°C Homo sapiens N-[5-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
2.1.2.2 0.0000011
-
 at pH 7.5 and 37°C Homo sapiens N-[8-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)octanoyl]-D-glutamic acid
2.1.2.2 0.0000019
-
 at pH 7.5 and 37°C Homo sapiens N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
2.1.2.2 0.0000049
-
 at pH 7.5 and 37°C Homo sapiens N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
2.1.2.2 0.0000079
-
 at pH 7.5 and 37°C Homo sapiens N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-D-glutamic acid