CYSLTR2 as a Radioligand Therapy Target
CYSLTR2, cysteinyl leukotriene receptor 2, is a cell-surface protein (membrane receptor). In Human Protein Atlas immunohistochemistry, CYSLTR2 staining is highest in thyroid cancer (100% of samples positive), prostate cancer (100% of samples positive) and pancreatic cancer (100% of samples positive). Published literature reports that CYSLTR2 internalizes after ligand binding, which helps retain a radionuclide inside tumor cells. Clinical status: Discovery-stage (no clinical drug program).
Is CYSLTR2 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 thyroid 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.
CYSLTR2 expression in cancer
Protein expression of CYSLTR2 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 | 1.00 | High | 100% |
| Prostate Cancer | 1.00 | High | 100% |
| Pancreatic Cancer | 0.94 | High | 100% |
| Colorectal Cancer | 0.92 | High | 100% |
| Gastric Cancer | 0.86 | High | 92% |
| Neuroendocrine Tumors | 0.83 | High | 100% |
| Breast Cancer | 0.83 | High | 92% |
| Liver Cancer | 0.81 | High | 100% |
| Ovarian Cancer | 0.75 | High | 92% |
| Endometrial Cancer | 0.67 | High | 100% |
| Lung Cancer | 0.61 | High | 91% |
| Kidney Cancer | 0.58 | High | 92% |
| Bladder Cancer | 0.48 | Medium | 64% |
| Cervical Cancer | 0.44 | Medium | 50% |
| Testicular Cancer | 0.39 | Medium | 58% |
| Head and Neck Cancer | 0.11 | Low | 33% |
| Skin Cancer | 0.06 | Low | 8% |
| Melanoma | 0.03 | Low | 9% |
Not detected by IHC in: lymphoma, glioma.
Is CYSLTR2 internalized?
Yes. High concentrations of LTs cause internalization and, in consequence, reduction in the number of receptors on the cell surface.
Sources: PMID 28477840. AI-extracted from abstracts, so verify before citing.
CYSLTR2 clinical trials
Discovery-stage (no clinical drug program). Nuclens hasn't indexed trials for CYSLTR2 yet. Search ClinicalTrials.gov for CYSLTR2 trials.
CYSLTR2 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 CYSLTR2 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
CYSLTR2 gene essentiality (DepMap)
CRISPR knockout effect across 1235 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.
Related thyroid cancer radioligand targets
c-MET (MET) · HER3 (ERBB3) · EPCAM · SSTR2 · EGFR · ITGAV · STEAP2 · FAP
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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.