TRPV2 as a Radioligand Therapy Target
TRPV2, transient receptor potential cation channel subfamily V member 2, is a cell-surface protein (membrane receptor). In Human Protein Atlas immunohistochemistry, TRPV2 staining is highest in melanoma (100% of samples positive), ovarian cancer (100% of samples positive) and gastric cancer (88% of samples positive). Evidence on whether TRPV2 internalizes is mixed. Clinical status: Discovery-stage (no clinical drug program).
Is TRPV2 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: High IHC staining in melanoma, 100% of samples positive.
- ⚠️ Internalization: Mixed evidence.
- ⚠️ Clinical precedent: Discovery-stage (no clinical drug program)
- ❔ Shedding: Not yet assessed.
- ❔ Normal-tissue dosimetry: Check kidney, liver, bone marrow and salivary expression in the Human Protein Atlas tissue atlas.
TRPV2 expression in cancer
Protein expression of TRPV2 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 |
|---|---|---|---|
| Melanoma | 1.00 | High | 100% |
| Ovarian Cancer | 0.91 | High | 100% |
| Gastric Cancer | 0.71 | High | 88% |
| Endometrial Cancer | 0.70 | High | 89% |
| Pancreatic Cancer | 0.67 | High | 90% |
| Colorectal Cancer | 0.64 | High | 100% |
| Breast Cancer | 0.58 | High | 91% |
| Thyroid Cancer | 0.50 | Medium | 100% |
| Neuroendocrine Tumors | 0.50 | Medium | 75% |
| Lung Cancer | 0.48 | Medium | 82% |
| Glioma | 0.47 | Medium | 75% |
| Cervical Cancer | 0.37 | Medium | 56% |
| Lymphoma | 0.36 | Medium | 73% |
| Bladder Cancer | 0.36 | Medium | 64% |
| Head and Neck Cancer | 0.33 | Medium | 67% |
| Skin Cancer | 0.28 | Medium | 58% |
| Prostate Cancer | 0.27 | Medium | 50% |
| Liver Cancer | 0.19 | Low | 33% |
| Kidney Cancer | 0.17 | Low | 33% |
| Testicular Cancer | 0.06 | Low | 17% |
Is TRPV2 internalized?
Uncertain. Insufficient literature found.
Sources: PMID 31896817 · PMID 23542034. AI-extracted from abstracts, so verify before citing.
TRPV2 clinical trials
Discovery-stage (no clinical drug program). Nuclens hasn't indexed trials for TRPV2 yet. Search ClinicalTrials.gov for TRPV2 trials.
TRPV2 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 TRPV2 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
TRPV2 gene essentiality (DepMap)
CRISPR knockout effect across 1256 cancer cell lines: -0.16 (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 melanoma radioligand targets
HER3 (ERBB3) · c-MET (MET) · STEAP2 · SSTR2 · B7-H3 (CD276) · ITGAV · TMEFF2 · FAP
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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.