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Target intelligence / Profile preview
5,10-Methenyltetrahydrofolate synthetase (MTHFS)
- Target
- MTHFS
- Molecular classification
- Enzyme
01
Overview
5,10-Methenyltetrahydrofolate synthetase (MTHFS) is an ATP- and Mg²⁺-dependent enzyme that irreversibly catalyzes the conversion of 5-formyltetrahydrofolate (a folate storage form) to 5,10-methenyltetrahydrofolate, a key intermediate in one-carbon metabolism essential for DNA synthesis, DNA methylation, and neurotransmitter biosynthesis[1][3][5]. MTHFS plays a critical role in regulating cellular folate pools and is required for maintaining nucleotide biosynthesis and methylation reactions, especially in rapidly dividing cells and during neurodevelopment. Genetic variants or altered expression of MTHFS are associated with increased risk or development of cancers, neurological disorders, and other diseases linked to impaired one-carbon metabolism. Experimental evidence supports its role as a potential therapeutic target and biomarker for diseases modulated by folate metabolism[1][3][5].
- Other names
- 5-formyltetrahydrofolate cyclo-ligaseMethenyl-THF synthetase5,10-methenyl-tetrahydrofolate synthetaseHsT19268NEDMEHMMTHFS
02
Mechanism of action
Inhibition of folate metabolism Modulation of purine biosynthesis by altering 10-formyltetrahydrofolate availability[5]
03
Biological functions
One-carbon metabolismFolate turnover and homeostasisDNA synthesisDNA methylationPurine biosynthesisNeurotransmitter synthesis
04
Disease associations
Cancer (notably non-Hodgkin lymphoma and ovarian carcinoma)[1][3]Neurological disorders (including cerebral folate deficiency syndrome, epilepsy, spasticity, hypomyelination)[3]Renal disease susceptibility[1]Growth retardation
05
Safety considerations
Potential for folate depletion from excessive MTHFS activity[1][3]Therapeutic targeting may affect DNA synthesis, methylation, and neurotransmitter production[3][5]Essentiality in mammals—complete deficiency is lethal (as evidenced in mice)[3][5]Non-specificity and systemic effects on one-carbon metabolism may present challenges
06
Interacting drugs
Antifolate agents (purine synthesis inhibitors)[5]
1 more in the full profile.
07
Biomarkers
MTHFS activity or expression level as indicator for folate cycle status[1][3][5]Genetic polymorphisms of MTHFS in risk assessment (e.g., non-Hodgkin lymphoma, renal disease susceptibility)[1][3]
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