Target intelligence / Profile preview

Transferrin receptor 1 (TfR1) and Transferrin (TfR1 (for receptor), TF (for protein))

Target
TfR1 (for receptor), TF (for protein)
Molecular classification
Transporter (plasma protein), Receptor (cell surface glycoprotein), Membrane protein
01

Overview

The transferrin pathway consists of transferrin, a glycoprotein produced in the liver, which binds and transports iron through the blood to cells. Cellular uptake of iron occurs when transferrin interacts with transferrin receptor 1 (TfR1) on cell surfaces, starting receptor-mediated endocytosis. In the acidic environment of the endosome, transferrin releases iron, which is then utilized or stored by the cell. Iron-free transferrin (apotransferrin) is recycled to the plasma to begin another transport cycle. This system maintains iron homeostasis, supports cellular metabolism, and contributes to immunity by limiting iron availability to pathogens. Dysregulation is associated with anemia, cancer, infection, and other diseases.

Other names
TransferrinSerotransferrinTFApotransferrin (iron-free form)Ovotransferrin (in egg white)Transferrin receptor 1TfR1CD71
02

Mechanism of action

Drugs may block or mimic transferrin binding to TfR1 to inhibit iron uptake by cancer cells or microorganisms. Chelators remove iron, reducing transferrin’s ability to deliver iron. ADCs targeting TfR1 deliver cytotoxic agents into cancer cells via receptor-mediated endocytosis.

03

Biological functions

Iron transport and deliveryRegulation of iron homeostasisPrevents formation of reactive oxygen speciesCellular iron uptake (via receptor-mediated endocytosis)Innate immune response (restricts iron for pathogens)
04

Disease associations

Cancer (upregulated TfR1, targeted in therapy)Iron deficiency anemia, atransferrinemiaInflammation, as transferrin levels decreaseInfection (immune response regulator)Cardiovascular disease (role in iron transport)
05

Safety considerations

Iron deprivation or overload due to dysregulation can cause toxicity or deficiencyTargeting TfR1 in therapy may affect normal cells, especially erythroid precursorsOff-target effects in cardiovascular, liver, or immune function
06

Interacting drugs

Iron chelators (e.g. deferoxamine)

3 more in the full profile.

07

Biomarkers

Serum transferrin (TF) levelsSoluble transferrin receptor (sTfR): biomarker for iron deficiency and erythropoietic activityCarbohydrate-deficient transferrin: marker for alcoholic liver disease

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