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. Author manuscript; available in PMC: 2013 Oct 23.
Published in final edited form as: Nat Rev Cancer. 2013 Jul 4;13(8):572–583. doi: 10.1038/nrc3557

Table 3.

Drug targets in one carbon metabolism

Enzymes Compounds Status
Methotetrahydrofolate Reductase Methotrexate, Pemetrexed Approved for multiple cancers
Thymidylate Synthase 5-Fluorouracil (5-FU) Approved for multiple cancers most notably Colorectal Cancer
Ribonucleotide Reductase Gemcitabine Approved for multiple cancers most notably Pancreatic Cancer
Polyamine Inhibitors Various Clinical trials ongoing
DNA Methyltransferase Inihibitors Azanucleosides Approved for Myeloid Leukemias
Histone Methyltransferase Inhibitors Various (SAM-analogs) Clinical trials ongoing
Histone Demethylase Inhibitors Various Preclinical studies
Ornithine Decarboxylase 2-difluoromethyl ornithine (DMFO) Preclinical studies
S-adenosyl decarboxylase inhibitors methylglyoxal bis(guanylhydrazone) (MGBG), 4-amidinoindydrazone-1-(SAM486A) Preclinical studies