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Literature summary extracted from

  • McGuire, J.J.; Hart, B.P.; Haile, W.H.; Rhee, M.S.; Galivan, J.; Coward, J.K.
    DL-beta,beta-Difluoroglutamic acid mediates position-dependent enhancement or termination of pteroylpoly(glutamate)synthesis catalyzed by folylpolyglutamate synthetase (1995), Arch. Biochem. Biophys., 321, 319-328.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
6.3.2.17 3,3-difluoroglutamate i.e. beta,beta-difluoroglutamate??, , the effect on polyglutamylation is dependent on its position relative to the point of L-Glu ligation. When beta,beta-difluoroglutamate is the acceptor amino acid, i.e. point of attachment. Ligation of Glu is enhanced. When beta,beta-difluoroglutamate is one residue distal to the acceptor amino acid, further elongation is blocked Homo sapiens
6.3.2.17 3,3-difluoroglutamate i.e. beta,beta-difluoroglutamate??, , the effect on polyglutamylation is dependent on its position relative to the point of L-Glu ligation. When beta,beta-difluoroglutamate is the acceptor amino acid, i.e. point of attachment. Ligation of Glu is enhanced. When beta,beta-difluoroglutamate is one residue distal to the acceptor amino acid, further elongation is blocked Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.3.2.17 3,3-Difluoroglutamic acid i.e. beta,beta-difluoroglutamate, , the effect on polyglutamylation is dependent on its position relative to the point of L-Glu ligation. When beta,beta-difluoroglutamate is the acceptor amino acid, i.e. point of attachment. Ligation of Glu is enhanced. When beta,beta-difluoroglutamate is one residue distal to the acceptor amino acid, further elongation is blocked Homo sapiens
6.3.2.17 3,3-Difluoroglutamic acid i.e. beta,beta-difluoroglutamate, , the effect on polyglutamylation is dependent on its position relative to the point of L-Glu ligation. When beta,beta-difluoroglutamate is the acceptor amino acid, i.e. point of attachment. Ligation of Glu is enhanced. When beta,beta-difluoroglutamate is one residue distal to the acceptor amino acid, further elongation is blocked Rattus norvegicus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
6.3.2.17 0.002
-
 5,6,7,8-tetrahydropteroyl-Glu4 7,8-dihydropteroyl-Glu Homo sapiens
6.3.2.17 0.0031
-
 3,3-difluoromethotrexate
-
 Rattus norvegicus
6.3.2.17 0.004
-
 aminopterin
-
 Homo sapiens
6.3.2.17 0.0054
-
 3,3-difluoromethotrexate
-
 Homo sapiens
6.3.2.17 0.019
-
 methotrexate
-
 Homo sapiens
6.3.2.17 0.025
-
 aminopterin pteroyl-3,3-difluoroglutamate Homo sapiens
6.3.2.17 0.047
-
 methotrexate
-
 Homo sapiens
6.3.2.17 0.132
-
 pteroyl-Glu
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
6.3.2.17 Homo sapiens
-
-
-
6.3.2.17 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
6.3.2.17 CEM cell
-
 Homo sapiens
-
6.3.2.17 liver
-
 Homo sapiens
-
6.3.2.17 liver
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.3.2.17 ATP + 3,3-difluoromethotrexate + L-glutamate
-
 Homo sapiens ?
-
 ?
6.3.2.17 ATP + 3,3-difluoromethotrexate + L-glutamate
-
 Rattus norvegicus ?
-
 ?
6.3.2.17 ATP + 3,5-difluoromethotrexate + Glu
-
 Homo sapiens ADP + phosphate + 3,5-difluoromethotrexyl-Glu
-
 ?
6.3.2.17 ATP + 3,5-difluoromethotrexate + Glu
-
 Rattus norvegicus ADP + phosphate + 3,5-difluoromethotrexyl-Glu
-
 ?
6.3.2.17 ATP + 3,5-difluoropteroyl-Glu + Glu
-
 Homo sapiens ADP + phosphate + 3,5-difluoropteroyl-Glu2
-
 ?
6.3.2.17 ATP + 3,5-difluoropteroyl-Glu + Glu
-
 Rattus norvegicus ADP + phosphate + 3,5-difluoropteroyl-Glu2
-
 ?
6.3.2.17 ATP + 7,8-dihydropteroyl-Glun + Glu n: 1 Homo sapiens ADP + phosphate + 7,8-dihydropteroyl-Glun+1
-
 ?
6.3.2.17 ATP + 7,8-dihydropteroyl-Glun + Glu n: 1 Rattus norvegicus ADP + phosphate + 7,8-dihydropteroyl-Glun+1
-
 ?
6.3.2.17 ATP + aminopterin + Glu
-
 Homo sapiens ADP + phosphate + aminopteryl-Glu
-
 ?
6.3.2.17 ATP + aminopterin + Glu
-
 Rattus norvegicus ADP + phosphate + aminopteryl-Glu
-
 ?
6.3.2.17 ATP + methotrexate + 3,3-difluoroglutamate
-
 Rattus norvegicus ADP + phosphate + methotrexyl-3,3-difluoroglutamate
-
 ?
6.3.2.17 ATP + methotrexate + Glu
-
 Homo sapiens ADP + phosphate + methotrexyl-Glu
-
 ?
6.3.2.17 ATP + pteroyl-Glu + Glu n: 1, i.e. pteroylmonoglutamate, folic acid Homo sapiens ADP + phosphate + pteroylmonoglutamyl-Glu
-
 ?
6.3.2.17 ATP + pteroyl-Glu + Glu n: 1, i.e. pteroylmonoglutamate, folic acid Rattus norvegicus ADP + phosphate + pteroylmonoglutamyl-Glu
-
 ?