GPR37 as a Radioligand Therapy Target
GPR37, G protein-coupled receptor 37, is a cell-surface protein (GPCR). In Human Protein Atlas immunohistochemistry, GPR37 staining is highest in thyroid cancer (50% of samples positive), head and neck cancer (25% of samples positive) and melanoma (25% of samples positive). Published literature reports that GPR37 internalizes after ligand binding, which helps retain a radionuclide inside tumor cells. Clinical status: Discovery-stage (no clinical drug program).
Is GPR37 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: Medium IHC staining in thyroid cancer, 50% of samples positive.
- ✅ Internalization: Reported to internalize, which favors radionuclide retention.
- ⚠️ 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.
GPR37 expression in cancer
Protein expression of GPR37 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 |
|---|---|---|---|
| Thyroid Cancer | 0.25 | Medium | 50% |
| Head and Neck Cancer | 0.08 | Low | 25% |
| Melanoma | 0.08 | Low | 25% |
| Kidney Cancer | 0.03 | Low | 8% |
| Lung Cancer | 0.03 | Low | 8% |
| Glioma | 0.03 | Low | 8% |
Not detected by IHC in: skin cancer, colorectal cancer, ovarian cancer, lymphoma, breast cancer, bladder cancer, neuroendocrine tumors, cervical cancer, pancreatic cancer, prostate cancer, gastric cancer, testicular cancer, endometrial cancer, liver cancer.
Is GPR37 internalized?
Yes. The abstract states that 'prosaptide... promoted the endocytosis of GPR37 and GPR37L1,' indicating that binding leads to receptor internalization.
Sources: PMID 25130661 · PMID 23690594 · PMID 23398388. AI-extracted from abstracts, so verify before citing.
GPR37 clinical trials
Discovery-stage (no clinical drug program). Nuclens hasn't indexed trials for GPR37 yet. Search ClinicalTrials.gov for GPR37 trials.
GPR37 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 GPR37 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
GPR37 gene essentiality (DepMap)
CRISPR knockout effect across 1258 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.
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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.