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TitleInternalization of methotrexate conjugates by folate receptor-α
Author(s)Nogueira, E.
Passos, M.
Azóia, Nuno G.
Antunes, Egipto
Loureiro, Ana
Guimarães, Diana Isabel Pereira
Jennifer Noro
Rollett, Alexandra
Guebitz, Georg M.
Cavaco-Paulo, Artur
Issue date19-Nov-2018
PublisherAmerican Chemical Society
CitationNogueira, E.; Passos, M.; Azoia, Nuno G.; Antunes, Egipto; Loureiro, Ana; Guimarães, Diana Isabel Pereira; Jennifer Noro; Rollett, Alexandra; Guebitz, Georg M.; Cavaco-Paulo, Artur, Internalization of methotrexate conjugates by folate receptor-α. Biochemistry, 57(49), 6780-6786, 2018
Abstract(s)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 accelerated if additional mechanistic data becomes available. In this work, we used two fluorescent-labeled conjugates of methotrexate, differently linked at the terminal groups, to clarify the uptake mechanism by the folate receptor-α. The results demonstrate the importance of methotrexate amino groups in the interaction with the folate receptor-α.
Publisher version
AccessOpen access
Appears in Collections:CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series

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