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Dihydrofolate reductase inhibitor

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Title: Dihydrofolate reductase inhibitor  
Author: World Heritage Encyclopedia
Language: English
Subject: Antifolate, Nitrofuran, Thymidylate synthase inhibitor, Ribonucleotide reductase inhibitor, COMT inhibitor
Collection: Dihydrofolate Reductase Inhibitors
Publisher: World Heritage Encyclopedia

Dihydrofolate reductase inhibitor

A dihydrofolate reductase inhibitor (DHFR 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:


  1. ^ Huennekens FM (1994). "The methotrexate story: a paradigm for development of cancer chemotherapeutic agents". Adv. Enzyme Regul. 34: 397–419.  
  2. ^ McGuire JJ (2003). "Anticancer antifolates: current status and future directions". Curr. Pharm. Des. 9 (31): 2593–613.  
  3. ^ Hawser S, Lociuro S, Islam K (March 2006). "Dihydrofolate reductase inhibitors as antibacterial agents". Biochem. Pharmacol. 71 (7): 941–8.  
  4. ^ Mui EJ, Schiehser GA, Milhous WK, et al. (2008). Matlashewski, Greg, ed. In Vitro and In Vivo"Toxoplasma gondii"Novel Triazine JPC-2067-B Inhibits . PLoS Negl Trop Dis 2 (3): e190.  
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