Inhibitors | Comment | Organism | Structure |
---|---|---|---|
lometrexol | competitive inhibition of murine MTHFS in vitro | Homo sapiens | |
lometrexol | competitive inhibition of murine MTHFS in vitro | Mus musculus | |
LY309887 | competitive inhibition of murine MTHFS in vitro | Homo sapiens | |
LY309887 | competitive inhibition of murine MTHFS in vitro | Mus musculus | |
additional information | inhibition mechanism overview | Homo sapiens | |
pemetrexed | competitive inhibition of murine MTHFS in vitro | Homo sapiens | |
pemetrexed | competitive inhibition of murine MTHFS in vitro | Mus musculus | |
[6R]-10-formyltetrahydrofolate | - |
Mus musculus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cytoplasm | - |
Mus musculus | 5737 | - |
cytoplasm | - |
Homo sapiens | 5737 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + 5-formyltetrahydrofolate | Mus musculus | - |
ADP + phosphate + 5,10-methenyltetrahydrofolate | - |
? | |
ATP + 5-formyltetrahydrofolate | Homo sapiens | - |
ADP + phosphate + 5,10-methenyltetrahydrofolate | - |
? | |
additional information | Homo sapiens | increased MTHFS expression affects the efficacy of the glycinamide ribonucleotide formyltransferase inhibitor LY309887, overview. SH-SY5Y neuroblastoma with increased MTHFS expression display a 4fold resistance to the GARFT inhibitor LY309887, but do not exhibit resistance to the thymidylate synthase inhibitor Pemetrexed. | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Mus musculus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
SH-SY5Y cell | a neuroblastoma cell line | Mus musculus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + 5-formyltetrahydrofolate | - |
Mus musculus | ADP + phosphate + 5,10-methenyltetrahydrofolate | - |
? | |
ATP + 5-formyltetrahydrofolate | - |
Homo sapiens | ADP + phosphate + 5,10-methenyltetrahydrofolate | - |
? | |
additional information | increased MTHFS expression affects the efficacy of the glycinamide ribonucleotide formyltransferase inhibitor LY309887, overview. SH-SY5Y neuroblastoma with increased MTHFS expression display a 4fold resistance to the GARFT inhibitor LY309887, but do not exhibit resistance to the thymidylate synthase inhibitor Pemetrexed. | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
5,10-Methenyltetrahydrofolate synthetase | - |
Mus musculus |
5,10-Methenyltetrahydrofolate synthetase | - |
Homo sapiens |
MTHFS | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Mus musculus |
37 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Mus musculus | |
ATP | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00015 | - |
[6R]-10-formyltetrahydrofolate | - |
Mus musculus | |
0.006 | - |
LY309887 | - |
Mus musculus | |
0.009 | - |
lometrexol | - |
Mus musculus | |
0.048 | - |
pemetrexed | - |
Mus musculus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.014 | - |
wild-type SH-SY5Y cells | Homo sapiens | LY309887 | |
0.029 | - |
recombinant SH-SY5Y cells overexpressing MTHFS | Homo sapiens | LY309887 | |
0.033 | - |
wild-type SH-SY5Y cells | Homo sapiens | pemetrexed | |
0.045 | - |
recombinant SH-SY5Y cells overexpressing MTHFS | Homo sapiens | pemetrexed | |
0.223 | - |
recombinant SH-SY5Y cells overexpressing MTHFS | Homo sapiens | lometrexol | |
0.303 | - |
wild-type SH-SY5Y cells | Homo sapiens | lometrexol |
Organism | Comment | Expression |
---|---|---|
Homo sapiens | 5,10-methenyltetrahydrofolate synthetase expression is upregulated in tumors | up |
General Information | Comment | Organism |
---|---|---|
metabolism | the enzyme is part of the folate-dependent one-carbon metabolism in the cytoplasm, overview | Mus musculus |
metabolism | the enzyme is part of the folate-dependent one-carbon metabolism in the cytoplasm, overview | Homo sapiens |