HTR2B as a Radioligand Therapy Target
HTR2B, 5-hydroxytryptamine receptor 2B, is a cell-surface protein (GPCR). In Human Protein Atlas immunohistochemistry, HTR2B staining is highest in breast cancer (92% of samples positive), pancreatic cancer (80% of samples positive) and bladder cancer (83% of samples positive). Evidence on whether HTR2B internalizes is mixed. Clinical status: Clinical-stage (up to phase 2, any modality).
Is HTR2B 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, 92% of samples positive.
- ⚠️ Internalization: Mixed evidence.
- ✅ Clinical precedent: Clinical-stage (up to phase 2, any modality)
- ❔ Shedding: Not yet assessed.
- ❔ Normal-tissue dosimetry: Check kidney, liver, bone marrow and salivary expression in the Human Protein Atlas tissue atlas.
HTR2B expression in cancer
Protein expression of HTR2B 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 | 0.83 | High | 92% |
| Pancreatic Cancer | 0.63 | High | 80% |
| Bladder Cancer | 0.56 | High | 83% |
| Colorectal Cancer | 0.55 | High | 73% |
| Gastric Cancer | 0.52 | High | 64% |
| Cervical Cancer | 0.42 | Medium | 73% |
| Endometrial Cancer | 0.42 | Medium | 75% |
| Lung Cancer | 0.42 | Medium | 67% |
| Head and Neck Cancer | 0.42 | Medium | 50% |
| Ovarian Cancer | 0.36 | Medium | 58% |
| Neuroendocrine Tumors | 0.33 | Medium | 50% |
| Thyroid Cancer | 0.25 | Medium | 25% |
| Liver Cancer | 0.17 | Low | 20% |
| Prostate Cancer | 0.12 | Low | 36% |
| Kidney Cancer | 0.12 | Low | 27% |
| Testicular Cancer | 0.08 | Low | 13% |
| Skin Cancer | 0.03 | Low | 8% |
Not detected by IHC in: lymphoma, melanoma, glioma.
Is HTR2B internalized?
Uncertain. Insufficient literature found.
HTR2B clinical trials
Clinical-stage (up to phase 2, any modality). Nuclens hasn't indexed trials for HTR2B yet. Search ClinicalTrials.gov for HTR2B trials.
HTR2B 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 HTR2B in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
HTR2B gene essentiality (DepMap)
CRISPR knockout effect across 1258 cancer cell lines: 0.00 (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.
See how HTR2B ranks against 15,000 targets for your indication.
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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.