Publications in International Journals / Series (Article (International))

Internalization of methotrexate conjugates by folate receptor-α

  • Biochemistry, 57(49), 6780-6786, 2018

Publisher: American Chemical Society


The folate antagonist methotrexate is a cytotoxic drug used in the treatment of several cancer types. Methotrexate entry into the cell is mediated by two main transport systems: the reduced folate carrier and membrane-associated folate receptors. These transporters differ considerably in their mechanism of (anti)folate uptake, substrate specificity and tissue specificity. Although the mechanism of action of the reduced folate carrier is fairly well-established, that of the folate receptor has remained doubtful. The development of specific folate receptor-targeted antifolates would be accelerat ...

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