TFR1

Transferrin receptor protein 1

Score: 0.590 Price: $0.59 Low Druggability Status: active Wiki: TFR1

🧠 Neurodegeneration

HYPOTHESES

PAPERS

KG EDGES

316

DEBATES

3D Protein Structure

🧬 TFR1 — PDB 1CX8 Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability

Low

Score: 0.44

Clinical Stage

Approved

Target Class

Receptor

Safety

0.50

Druggability Analysis

Drug Development0.60

Structural Tractability0.70

Target Class0.70

Safety Profile0.50

Key Metrics

PDB Structures:

Known Drugs:

Approved:

In Clinical Trials:

Drug Pipeline (2 compounds)

Therapeutic Areas:

Parkinson's disease Alzheimer's disease Neurodegeneration Iron overload disorders Drug delivery to CNS Ferroptosis-related diseases Neuroinflammation

Druggability Rationale: TFR1 is highly druggable (0.80 score) due to its cell-surface receptor localization, well-characterized structure (4 PDB entries at 1.85 Å resolution), and validated mechanism with approved iron chelators and clinical-stage antibodies. The receptor's critical role in iron homeostasis and established pharmacology via both small-molecule and biologic modalities supports therapeutic tractability.

Mechanism: Monoclonal antibodies targeting receptor or iron chelation affecting iron uptake

Drug Pipeline (2 compounds)

Known Drugs:

Deferasirox (Approved) — Iron chelation

Anti-TfR1 antibodies (Clinical trials) — Drug delivery

Structural Data:

PDB (4) ✓AlphaFold ✓Cryo-EM ✓

3S9L 3S9M 3S9N 6S9J

UniProt: P02786

Binding Pocket Analysis:

Structural data reveals a well-defined extracellular binding region suitable for antibody epitope targeting (PDB: 3S9L-3S9N, 6S9J); the iron-binding pocket within the transferrin-TFR1 complex (1.85 Å resolution) provides a validated site for small-molecule iron chelators to modulate receptor-ligand interactions and downstream iron uptake.

🧬 3D Protein Structure

🧬 TFR1 — PDB 1CX8 Click to expand interactive 3D viewer

Experimental structure from RCSB PDB | Powered by Mol* | Rotate: click+drag | Zoom: scroll

Selectivity & Safety Considerations

TFR1 is ubiquitously expressed across tissues, presenting selectivity challenges for systemic approaches; however, monoclonal antibodies offer improved selectivity through epitope-specific targeting, while brain delivery can be achieved via BBB-penetrant antibodies or transferrin conjugates. Iron chelators targeting TFR1-mediated uptake may show off-target effects on systemic iron metabolism and require careful dose titration.