KISS1R as a Radioligand Therapy Target
KISS1R, KISS1 receptor, is a cell-surface protein (GPCR). In Human Protein Atlas immunohistochemistry, KISS1R staining is highest in thyroid cancer (100% of samples positive), endometrial cancer (100% of samples positive) and melanoma (100% of samples positive). Evidence on whether KISS1R internalizes is mixed. Clinical status: Discovery-stage (no clinical drug program).
Is KISS1R 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: 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.
KISS1R expression in cancer
Protein expression of KISS1R 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 | 0.89 | High | 100% |
| Endometrial Cancer | 0.81 | High | 100% |
| Melanoma | 0.78 | High | 100% |
| Kidney Cancer | 0.78 | High | 92% |
| Liver Cancer | 0.76 | High | 82% |
| Bladder Cancer | 0.72 | High | 100% |
| Testicular Cancer | 0.67 | High | 91% |
| Colorectal Cancer | 0.64 | High | 100% |
| Pancreatic Cancer | 0.61 | High | 82% |
| Gastric Cancer | 0.58 | High | 82% |
| Breast Cancer | 0.57 | High | 90% |
| Neuroendocrine Tumors | 0.50 | Medium | 100% |
| Head and Neck Cancer | 0.50 | Medium | 75% |
| Prostate Cancer | 0.47 | Medium | 80% |
| Lymphoma | 0.46 | Medium | 82% |
| Ovarian Cancer | 0.44 | Medium | 83% |
| Lung Cancer | 0.44 | Medium | 83% |
| Skin Cancer | 0.33 | Medium | 46% |
| Glioma | 0.27 | Medium | 40% |
| Cervical Cancer | 0.15 | Low | 27% |
Is KISS1R internalized?
Uncertain. Insufficient literature found.
Sources: PMID 41774810 · PMID 25765628 · PMID 25563181 · PMID 24295737 · PMID 21285314. AI-extracted from abstracts, so verify before citing.
KISS1R clinical trials
Discovery-stage (no clinical drug program). Nuclens hasn't indexed trials for KISS1R yet. Search ClinicalTrials.gov for KISS1R trials.
KISS1R 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 KISS1R in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
KISS1R gene essentiality (DepMap)
CRISPR knockout effect across 1235 cancer cell lines: -0.02 (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
See all radioligand therapy targets in thyroid 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.