Tag: DHFR

Talotrexin, A RFC Specific Inhibitor, Targets DHFR to Inhibit Tumor Growth

In this article, we will introduce a potent RFC (reduced folate carrier) specific inhibitor Talotrexin (PT523). Talotrexin, an analog of Aminopterin, is a nonpolyglutamatable classic antifolate. Additionally, it selectively inhibits RFC transport. Mammals cannot synthesize folates de novo, their cellular uptake from the extracellular milieu is essential. Besides, The...

TNP-351, an Antifolate, is a Dihydrofolate Reductase (DHFR) Inhibitor

Antifolates are a class of antimetabolite medications that block the actions of folic acid. Antimalarial antifolates have been central for prophylaxis and treatment of malaria. The success of antifolates in the treatment of tumors also leads to the use of this class of drugs in the treatment of other...