Application | Comment | Organism |
---|---|---|
medicine | the enzyme inhibition can be useful for cancer chemotherapy | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression in Sf9 insect cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
methotrexate-phosphinate | 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 | Homo sapiens | |
methotrexate-phosphonate | IC50 0.00012 mM, at fixed substrate and recombinant enzyme concentrations | Homo sapiens | |
additional information | no inhibition by methotrexate in the CCRF-CEM R2 cell subline | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | the enzyme synthesizes folate and antifolate poly(gamma-glutamate) metabolites | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
human | - |
Purification (Comment) | Organism |
---|---|
ammonium sulfate fractionation and chromatography on BioGel A-0.5M, recombinant enzyme | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
CCRF-CEM cell | T-lymphoblastic leukemia line, wild type cell line and its methrotrexate transport-deficient subline R2 | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + methotrexate-Glu + L-glutamate | - |
Homo sapiens | ADP + methotrexate-Glu2 + phosphate | - |
? | |
ATP + methotrexate-phosphinate + L-glutamate | - |
Homo sapiens | ? | - |
? | |
ATP + methotrexate-phosphonate + L-glutamate | - |
Homo sapiens | ? | - |
? | |
additional information | the enzyme synthesizes folate and antifolate poly(gamma-glutamate) metabolites | Homo sapiens | ? | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000031 | - |
methotrexate-phosphinate | Kis value, with methrotrexate as variable substrate, for recombinant enzyme | Homo sapiens | |
0.000056 | - |
methotrexate-phosphinate | Kii value, with methotrexate as variable substrate, for recombinant enzyme | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000008 | - |
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 | Homo sapiens | methotrexate-phosphinate | |
0.00012 | - |
IC50 0.00012 mM, at fixed substrate and recombinant enzyme concentrations | Homo sapiens | methotrexate-phosphonate |