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 |