GRPR as a Radioligand Therapy Target
GRPR, gastrin releasing peptide receptor, is a cell-surface protein (GPCR). No tumor protein staining is recorded for it in Human Protein Atlas immunohistochemistry. Evidence on whether GRPR internalizes is mixed. Clinical status: Discovery-stage (no clinical drug program), with 1 active clinical trial.
Is GRPR 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: No tumor staining in HPA immunohistochemistry.
- ⚠️ 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.
GRPR expression in cancer
No Human Protein Atlas tumor immunohistochemistry data is available for GRPR.
Is GRPR internalized?
Uncertain. Insufficient literature found.
Sources: PMID 42010078 · PMID 41756872 · PMID 41701408 · PMID 41231375 · PMID 41217470. AI-extracted from abstracts, so verify before citing.
GRPR clinical trials
Discovery-stage (no clinical drug program). 1 active trial reference GRPR (ClinicalTrials.gov, accessed 2026-09-21).
GRPR 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 GRPR in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
GRPR gene essentiality (DepMap)
CRISPR knockout effect across 1257 cancer cell lines: 0.03 (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.