PDGFRA as a Radioligand Therapy Target
PDGFRA, platelet derived growth factor receptor alpha, is a cell-surface protein (membrane receptor). In Human Protein Atlas immunohistochemistry, PDGFRA staining is highest in glioma (33% of samples positive), melanoma (10% of samples positive) and ovarian cancer (8% of samples positive). Published literature reports that PDGFRA internalizes after ligand binding, which helps retain a radionuclide inside tumor cells. Clinical status: Clinical-stage (up to phase 3, any modality).
Is PDGFRA a good radioligand therapy target?
Scored against the six criteria that decide whether a protein can become a radioligand therapy:
- ✅ Cell-surface accessibility: Localized to the cell surface, so a radioligand can reach it from circulation.
- ⚠️ Tumor expression: Low IHC staining in glioma, 33% of samples positive.
- ✅ Internalization: Reported to internalize, which favors radionuclide retention.
- ✅ Clinical precedent: Clinical-stage (up to phase 3, any modality)
- ❔ Shedding: Not yet assessed.
- ❔ Normal-tissue dosimetry: Check kidney, liver, bone marrow and salivary expression in the Human Protein Atlas tissue atlas.
PDGFRA expression in cancer
Protein expression of PDGFRA across 20 cancer types from Human Protein Atlas immunohistochemistry. The score is a weighted staining intensity from 0 to 1; "% positive" is the share of patient samples with detectable staining.
| Cancer type | IHC score | Level | % positive |
|---|---|---|---|
| Glioma | 0.17 | Low | 33% |
| Melanoma | 0.07 | Low | 10% |
| Ovarian Cancer | 0.06 | Low | 8% |
| Testicular Cancer | 0.05 | Low | 14% |
| Bladder Cancer | 0.03 | Low | 9% |
Not detected by IHC in: skin cancer, colorectal cancer, head and neck cancer, lymphoma, breast cancer, kidney cancer, thyroid cancer, neuroendocrine tumors, cervical cancer, lung cancer, pancreatic cancer, prostate cancer, gastric cancer, endometrial cancer, liver cancer.
Is PDGFRA internalized?
Yes. We discovered that PDGFRA can be targeted to autophagic degradation by binding the autophagy cargo receptor SQSTM1.
Sources: PMID 38634484 · PMID 38113891 · PMID 38004483 · PMID 23127761 · PMID 18701889. AI-extracted from abstracts, so verify before citing.
PDGFRA clinical trials
Clinical-stage (up to phase 3, any modality). Nuclens hasn't indexed trials for PDGFRA yet. Search ClinicalTrials.gov for PDGFRA trials.
PDGFRA normal tissue expression
Normal-tissue expression in dose-limiting organs (kidney, liver, bone marrow, salivary glands) drives radioligand dosimetry risk. Nuclens is re-validating its normal-tissue values, so they are not shown here yet. See PDGFRA in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
PDGFRA gene essentiality (DepMap)
CRISPR knockout effect across 1258 cancer cell lines: -0.20 (not essential). Radioligands kill by radiation, not by blocking the target, so essentiality matters less than for inhibitors. A non-essential target can still be an excellent radioligand target.
Related glioma radioligand targets
EGFR · HER3 (ERBB3) · c-MET (MET) · ITGAV · B7-H3 (CD276) · SSTR2 · STEAP2 · FAP
See all radioligand therapy targets in glioma.
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Subcellular localization: UniProt via Open Targets (CC BY 4.0 / CC0). Tumor immunohistochemistry: Human Protein Atlas (CC BY-SA 4.0). Clinical trials: ClinicalTrials.gov (public domain). Gene essentiality: DepMap (CC BY 4.0). Internalization and shedding: AI-extracted from PubMed abstracts, so verify against the cited papers before relying on them. Nuclens is a first-pass triage layer, not a substitute for wet-lab validation or clinical dosimetry. Derived expression data on this page is shared under CC BY-SA 4.0.