VIPR1 as a Radioligand Therapy Target
VIPR1, vasoactive intestinal peptide receptor 1, is a cell-surface protein (GPCR). In Human Protein Atlas immunohistochemistry, VIPR1 staining is highest in breast cancer (100% of samples positive), pancreatic cancer (100% of samples positive) and head and neck cancer (100% of samples positive). Published literature reports that VIPR1 internalizes after ligand binding, which helps retain a radionuclide inside tumor cells. Clinical status: Discovery-stage (no clinical drug program).
Is VIPR1 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 breast cancer, 100% 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.
VIPR1 expression in cancer
Protein expression of VIPR1 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 |
|---|---|---|---|
| Breast Cancer | 0.61 | High | 100% |
| Pancreatic Cancer | 0.61 | High | 100% |
| Head and Neck Cancer | 0.58 | High | 100% |
| Ovarian Cancer | 0.58 | High | 100% |
| Neuroendocrine Tumors | 0.58 | High | 100% |
| Thyroid Cancer | 0.56 | High | 100% |
| Testicular Cancer | 0.56 | High | 100% |
| Endometrial Cancer | 0.53 | High | 100% |
| Prostate Cancer | 0.47 | Medium | 92% |
| Cervical Cancer | 0.47 | Medium | 83% |
| Skin Cancer | 0.46 | Medium | 100% |
| Liver Cancer | 0.44 | Medium | 92% |
| Lung Cancer | 0.43 | Medium | 100% |
| Colorectal Cancer | 0.42 | Medium | 100% |
| Bladder Cancer | 0.42 | Medium | 100% |
| Gastric Cancer | 0.41 | Medium | 89% |
| Melanoma | 0.36 | Medium | 82% |
| Kidney Cancer | 0.36 | Medium | 75% |
| Glioma | 0.27 | Medium | 50% |
| Lymphoma | 0.25 | Medium | 50% |
Is VIPR1 internalized?
Yes. VIPR1 and β2-adrenergic receptor (β2AR) both rapidly internalize after activation.
Sources: PMID 41654131 · PMID 37749347 · PMID 30008714 · PMID 27194157 · PMID 21492484. AI-extracted from abstracts, so verify before citing.
VIPR1 clinical trials
Discovery-stage (no clinical drug program). Nuclens hasn't indexed trials for VIPR1 yet. Search ClinicalTrials.gov for VIPR1 trials.
VIPR1 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 VIPR1 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
VIPR1 gene essentiality (DepMap)
CRISPR knockout effect across 1256 cancer cell lines: 0.05 (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 breast cancer radioligand targets
HER3 (ERBB3) · c-MET (MET) · FAP · HER2 (ERBB2) · STEAP2 · EGFR · B7-H3 (CD276) · SSTR2
See all radioligand therapy targets in breast cancer.
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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.