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September 11, 2024Drug Metabolism and Disposition

Functional characterizationof RFC and PCFT for antifolates accumulation in non-small cell lung cancer cells

Yuqing Wang Jun Luo Mengru Bai Zhiyuan Ma Ying Xu Dan Liu Huidi Jiang Shenglin Ma Shirong Zhang

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Abstract

Antifolates are important for chemotherapy in non-small cell lung cancer (NSCLC). They mainly rely on reduced folate carrier (RFC) and proton-coupled folate transporter (PCFT) to enter cells. PCFT is supposed to be the dominant transporter of the two in tumors as it operates optimally at acidic pH and has limited transport activity at physiological pH, whereas RFC operates optimally at neutral pH. In this study, we found RFC showed a slightly pH-dependent uptake of antifolates, with similar affinity values at pH 7.4 and 6.5. PCFT showed a highly pH-dependent uptake of antifolates with an optimum pH of 6.0 for pemetrexed and 5.5 for methotrexate. The

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Cite This Study

Wang et al. (2024) studied this question.

synapsesocial.com/papers/68e58cc8b6db643587528964 https://doi.org/10.1124/dmd.124.001872

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