Radioligand Therapy Targets in Glioma
We screened every cell-surface protein with tumor immunohistochemistry data in glioma (including glioblastoma (GBM)). 3,815 show detectable protein staining. Established and emerging radioligand targets expressed in glioma include EGFR, HER3 (ERBB3), ITGAV and B7-H3 (CD276). Below, we rank every candidate by tumor expression, internalization and clinical maturity.
Established and emerging radioligand targets in glioma
Targets already pursued with radioligands or other targeted modalities that show protein expression in glioma:
| Target | IHC in glioma | % positive | Internalizes |
|---|---|---|---|
| EGFR | High (0.81) | 92% | yes |
| HER3 (ERBB3) | High (0.75) | 100% | yes |
| ITGAV | High (0.72) | 100% | — |
| B7-H3 (CD276) | High (0.61) | 100% | — |
| STEAP2 | Medium (0.47) | 83% | — |
| c-MET (MET) | Medium (0.42) | 100% | yes |
| TMEFF2 | Medium (0.25) | 50% | — |
| SSTR2 | Medium (0.21) | 46% | yes |
| Nectin-4 (NECTIN4) | Low (0.08) | 17% | no |
| FAP | Low (0.08) | 17% | yes |
| Claudin 18.2 (CLDN18) | Low (0.06) | 8% | uncertain |
| KIT | Low (0.03) | 8% | no |
Top cell-surface targets for glioma radioligand therapy
A data-driven screen of every protein annotated as cell-surface. It deliberately surfaces novel, unvalidated candidates, so confirm localization and expression before prioritizing any of them.
| # | Target | IHC in glioma | % positive | Internalizes | Clinical stage |
|---|---|---|---|---|---|
| 1 | PTPRB protein tyrosine phosphatase receptor type B | High (0.88) | 100% | yes | Clinical |
| 2 | S1PR1 sphingosine-1-phosphate receptor 1 | High (0.86) | 100% | yes | Clinical |
| 3 | EGFR epidermal growth factor receptor | High (0.81) | 92% | yes | Clinical |
| 4 | AMFR autocrine motility factor receptor | High (0.97) | 100% | yes | Discovery |
| 5 | HER3 (ERBB3) erb-b2 receptor tyrosine kinase 3 | High (0.75) | 100% | yes | Clinical |
| 6 | IGF1R insulin like growth factor 1 receptor | High (0.72) | 100% | yes | Clinical |
| 7 | GPR139 G protein-coupled receptor 139 | High (0.89) | 100% | yes | Discovery |
| 8 | PTPN13 protein tyrosine phosphatase non-receptor type 13 | High (0.83) | 100% | yes | Discovery |
| 9 | NOTCH1 notch receptor 1 | High (0.64) | 100% | yes | Clinical |
| 10 | TREM1 triggering receptor expressed on myeloid cells 1 | High (0.77) | 100% | uncertain | Clinical |
| 11 | CHRNA7 cholinergic receptor nicotinic alpha 7 subunit | High (0.63) | 100% | yes | Clinical |
| 12 | PTGER4 prostaglandin E receptor 4 | High (0.93) | 100% | uncertain | Clinical |
| 13 | NR3C2 nuclear receptor subfamily 3 group C member 2 | High (0.75) | 100% | uncertain | Clinical |
| 14 | IL1R2 interleukin 1 receptor type 2 | High (0.58) | 100% | yes | Discovery |
| 15 | MAOB monoamine oxidase B | High (0.85) | 100% | — | Clinical |
| 16 | RNF43 ring finger protein 43 | High (0.97) | 100% | — | Discovery |
| 17 | c-MET (MET) MET proto-oncogene, receptor tyrosine kinase | Medium (0.42) | 100% | yes | Clinical |
| 18 | IRAK4 interleukin 1 receptor associated kinase 4 | High (0.58) | 100% | yes | Clinical |
| 19 | MMP10 matrix metallopeptidase 10 | High (0.97) | 100% | — | Discovery |
| 20 | NSD1 nuclear receptor binding SET domain protein 1 | High (1.00) | 100% | uncertain | Discovery |
| 21 | HMGB1 high mobility group box 1 | High (1.00) | 100% | — | Clinical |
| 22 | LIFR LIF receptor subunit alpha | High (0.69) | 92% | yes | Discovery |
| 23 | PCDHGC3 protocadherin gamma subfamily C, 3 | High (0.94) | 100% | — | Discovery |
| 24 | LDB2 LIM domain binding 2 | High (0.94) | 100% | — | Discovery |
| 25 | GBA1 glucosylceramidase beta 1 | High (0.97) | 100% | — | Clinical |
Internalizing receptors in glioma
Targets expressed in glioma that the literature reports internalize after ligand binding. Internalization traps the radionuclide inside the tumor cell, which matters most for β-emitters like 177Lu and for α-emitters like 225Ac:
PTPRB · S1PR1 · EGFR · AMFR · HER3 (ERBB3) · IGF1R · GPR139 · PTPN13 · NOTCH1 · CHRNA7 · IL1R2 · c-MET (MET)
Glioma targets already in clinical development
Targets with a clinical-stage drug program (any modality) that are also expressed in glioma. Clinical precedent lowers development risk but usually means more competition:
PTPRB · S1PR1 · EGFR · HER3 (ERBB3) · IGF1R · NOTCH1 · TREM1 · CHRNA7 · PTGER4 · NR3C2 · MAOB · c-MET (MET)
How these glioma targets are ranked
Candidates are limited to proteins annotated as cell-surface (UniProt via Open Targets), because a radioligand has to reach its target from circulation. They are ranked by Nuclens' radiopharmaceutical pre-screen: immunohistochemistry staining and patient-sample positivity in glioma, literature evidence of internalization and shedding, clinical maturity, and cancer association. It is a first-pass triage, not a substitute for wet-lab validation or dosimetry. For the full framework, see what makes a good radioligand therapy target and emerging radioligand targets beyond PSMA.
Rank glioma targets against your own criteria: isotope, organ limits, novelty.
Run a free glioma analysisRadioligand therapy targets in other cancers
- Prostate Cancer
- Neuroendocrine Tumors
- Lung Cancer
- Pancreatic Cancer
- Breast Cancer
- Ovarian Cancer
- Colorectal Cancer
- Kidney Cancer
- Bladder Cancer
- Gastric Cancer
- Liver Cancer
- Melanoma
- Head and Neck Cancer
- Thyroid Cancer
- Lymphoma
- Cervical Cancer
- Endometrial Cancer
- Skin Cancer
- Testicular Cancer
Data sources
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.