Dihydrofolate reductase inhibitor

A dihydrofolate reductase inhibitor is a molecule that inhibits the function of dihydrofolate reductase, and is a type of antifolate.

Since folate is needed by rapidly dividing cells to make thymine, this effect may be used to therapeutic advantage. For example, methotrexate is used as cancer chemotherapy because it can prevent neoplastic cells from dividing.^[1][2] Bacteria also need DHFR to grow and multiply and hence inhibitors selective for bacterial vs. host DHFR have found application as antibacterial agents.^[3]

Tetrahydrofolate synthesis pathway

A variety of drugs act as inhibitors of dihydrofolate reductase:

• the antibiotic trimethoprim and its derivatives brodimoprim, tetroxoprim, and iclaprim.
• the antimalarial drugs pyrimethamine and proguanil.
• the experimental new antimalarial drug JPC-2056, which may also be more effective and better tolerated than current treatments against toxoplasmosis.^[4]
• the chemotherapeutic agents methotrexate and pemetrexed. Methotrexate acts on this enzyme binding to it some 1000 times more tightly than folate itself.

References

1. ^ Huennekens FM (1994). "The methotrexate story: a paradigm for development of cancer chemotherapeutic agents". Adv. Enzyme Regul. 34: 397–419. doi:10.1016/0065-2571(94)90025-6. PMID 7942284. 
2. ^ McGuire JJ (2003). "Anticancer antifolates: current status and future directions". Curr. Pharm. Des. 9 (31): 2593–613. doi:10.2174/1381612033453712. PMID 14529544. 
3. ^ Hawser S, Lociuro S, Islam K (March 2006). "Dihydrofolate reductase inhibitors as antibacterial agents". Biochem. Pharmacol. 71 (7): 941–8. doi:10.1016/j.bcp.2005.10.052. PMID 16359642. 
4. ^ Mui EJ, Schiehser GA, Milhous WK, et al. (2008). Matlashewski, Greg. ed. "Novel Triazine JPC-2067-B Inhibits Toxoplasma gondii In Vitro and In Vivo". PLoS Negl Trop Dis 2 (3): e190. doi:10.1371/journal.pntd.0000190. PMC 2254147. PMID 18320016. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2254147. 

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