Antifolates are compounds that antagonise the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis. Consequently antifolates inhibit cell division, DNA/RNA synthesis and repair and protein synthesis. Some such as Proguanil, Pyrimethamine and Trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi. The majority of antifolates work by inhibiting dihydrofolate reductase (DHFR). Many are primarily DHFR inhibitors, but Raltitrexed is an inhibitor of thymidylate synthase, and Pemetrexed inhibits both and a third enzyme. Antifolates act specifically during DNA and RNA synthesis, and thus are cytotoxic during the S-phase of the cell cycle. Thus, they have a greater toxic effect on rapidly dividing cells.
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A calcium salt of levomefolic acid.
A classical multitargeted antifolate that inhibits multiple folate-requiring enzymes TS/DHFR/GARFT with Ki of 1.3/7.2/65 nM respectively; increases the cytotoxicity and antitumor activity of gemcitabine in HT29 colon carcinoma.
Arfolitixorin is an antifolate modulator drug candidate.
Pralatrexate is an antifolate that fuctions as a dihydrofolate reductase inhibitor for treatment of several malignancies.
The calcium salt of levomefolic acid that has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers.
Pemetrexed disodium is a classical multitargeted antifolate that inhibits multiple folate-requiring enzymes TS/DHFR/GARFT with Ki of 1.3/7.2/65 nM respectively; increases the cytotoxicity and antitumor activity of gemcitabine in HT29 colon carcinoma.
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