GPR143 as a Radioligand Therapy Target
GPR143, G protein-coupled receptor 143, is a cell-surface protein (GPCR). In Human Protein Atlas immunohistochemistry, GPR143 staining is highest in melanoma (75% of samples positive), breast cancer (100% of samples positive) and skin cancer (46% of samples positive). Evidence on whether GPR143 internalizes is mixed. Clinical status: Discovery-stage (no clinical drug program).
Is GPR143 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, 75% 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.
GPR143 expression in cancer
Protein expression of GPR143 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 | 0.69 | High | 75% |
| Breast Cancer | 0.50 | Medium | 100% |
| Skin Cancer | 0.39 | Medium | 46% |
| Prostate Cancer | 0.37 | Medium | 80% |
| Thyroid Cancer | 0.33 | Medium | 100% |
| Testicular Cancer | 0.33 | Medium | 67% |
| Pancreatic Cancer | 0.28 | Medium | 67% |
| Head and Neck Cancer | 0.25 | Medium | 75% |
| Neuroendocrine Tumors | 0.25 | Medium | 75% |
| Colorectal Cancer | 0.24 | Medium | 73% |
| Endometrial Cancer | 0.22 | Medium | 67% |
| Bladder Cancer | 0.22 | Medium | 58% |
| Kidney Cancer | 0.21 | Medium | 46% |
| Liver Cancer | 0.18 | Low | 36% |
| Ovarian Cancer | 0.17 | Low | 50% |
| Lung Cancer | 0.14 | Low | 33% |
| Cervical Cancer | 0.12 | Low | 36% |
| Glioma | 0.11 | Low | 33% |
| Gastric Cancer | 0.03 | Low | 9% |
| Lymphoma | 0.03 | Low | 8% |
Is GPR143 internalized?
Uncertain. Insufficient literature found.
GPR143 clinical trials
Discovery-stage (no clinical drug program). Nuclens hasn't indexed trials for GPR143 yet. Search ClinicalTrials.gov for GPR143 trials.
GPR143 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 GPR143 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
GPR143 gene essentiality (DepMap)
CRISPR knockout effect across 1250 cancer cell lines: 0.11 (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
See all radioligand therapy targets in melanoma.
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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.