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Literature summary for 6.3.3.2 extracted from
- 5,10-Methenyltetrahydrofolate synthetase activity is increased in tumors and modifies the efficacy of antipurine LY309887 (2009), Arch. Biochem. Biophys., 481, 145-150.
Inhibitors
| 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
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytoplasm | - |
Homo sapiens | 5737 | - |
| cytoplasm | - |
Mus musculus | 5737 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + 5-formyltetrahydrofolate | Homo sapiens | - |
ADP + phosphate + 5,10-methenyltetrahydrofolate | - |
? | |
| ATP + 5-formyltetrahydrofolate | Mus musculus | - |
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
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| SH-SY5Y cell | a neuroblastoma cell line | Mus musculus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + 5-formyltetrahydrofolate | - |
Homo sapiens | ADP + phosphate + 5,10-methenyltetrahydrofolate | - |
? | |
| ATP + 5-formyltetrahydrofolate | - |
Mus musculus | 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
| Synonyms | Comment | Organism |
|---|---|---|
| 5,10-Methenyltetrahydrofolate synthetase | - |
Homo sapiens |
| 5,10-Methenyltetrahydrofolate synthetase | - |
Mus musculus |
| MTHFS | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
| 37 | - |
assay at | Mus musculus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
| ATP | - |
Mus musculus | |
Ki Value [mM]
| 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 | 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 | |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Homo sapiens | 5,10-methenyltetrahydrofolate synthetase expression is upregulated in tumors | up |
General Information
| General Information | Comment | Organism |
|---|---|---|
| metabolism | the enzyme is part of the folate-dependent one-carbon metabolism in the cytoplasm, overview | Homo sapiens |
| metabolism | the enzyme is part of the folate-dependent one-carbon metabolism in the cytoplasm, overview | Mus musculus |
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