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. 2018 Oct 2;9(1):366–378. doi: 10.1007/s13346-018-0589-2

Table 2.

Overview and expression profiling and transport kinetic features of folate transporters

Cellular (anti) folate uptake systems
PCFT (proton-coupled folate transporter) RFC (reduced folate carrier) FR (folate receptor α,β,γ isoform)
Membrane orientation Transmembrane Transmembrane GPI - anchored
Localization Enterocytes Immune cells
Tumor cells
Kidney (FRα)
Tumor cells (FRα)
Myeloid cells/activated
Macrophages (FRβ)
Hematopoietic cells (FRγ, soluble, secreted form)
pH optimum 5.0–5.5 7.2–8.0 7.4–8.0
Affinity folic acid Km 1–5 μM Km 200–400 μM Kd 0.1–1 nM
Affinity 5-methyl-THF Km 2–10 μM Km 1–5 μM Kd 5–10 nM
Affinity MTX Km 2–10 μM Km 2–10 μM Kd 50–100 nM