GRIK1 as a Radioligand Therapy Target
GRIK1, glutamate ionotropic receptor kainate type subunit 1, is a cell-surface protein (membrane receptor). In Human Protein Atlas immunohistochemistry, GRIK1 staining is highest in thyroid cancer (100% of samples positive), head and neck cancer (100% of samples positive) and prostate cancer (100% of samples positive). Evidence on whether GRIK1 internalizes is mixed. Clinical status: Clinical-stage (up to phase 2, any modality).
Is GRIK1 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: 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.
GRIK1 expression in cancer
Protein expression of GRIK1 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 | 0.75 | High | 100% |
| Head and Neck Cancer | 0.67 | High | 100% |
| Prostate Cancer | 0.64 | High | 100% |
| Breast Cancer | 0.61 | High | 91% |
| Colorectal Cancer | 0.58 | High | 100% |
| Melanoma | 0.50 | Medium | 83% |
| Bladder Cancer | 0.47 | Medium | 92% |
| Gastric Cancer | 0.44 | Medium | 78% |
| Cervical Cancer | 0.42 | Medium | 91% |
| Ovarian Cancer | 0.42 | Medium | 92% |
| Glioma | 0.42 | Medium | 75% |
| Endometrial Cancer | 0.39 | Medium | 83% |
| Pancreatic Cancer | 0.39 | Medium | 75% |
| Testicular Cancer | 0.33 | Medium | 50% |
| Lung Cancer | 0.31 | Medium | 58% |
| Liver Cancer | 0.28 | Medium | 42% |
| Neuroendocrine Tumors | 0.25 | Medium | 50% |
| Skin Cancer | 0.24 | Medium | 55% |
| Kidney Cancer | 0.19 | Low | 42% |
| Lymphoma | 0.15 | Low | 36% |
Is GRIK1 internalized?
Uncertain. Insufficient literature found.
GRIK1 clinical trials
Clinical-stage (up to phase 2, any modality). Nuclens hasn't indexed trials for GRIK1 yet. Search ClinicalTrials.gov for GRIK1 trials.
GRIK1 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 GRIK1 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
GRIK1 gene essentiality (DepMap)
CRISPR knockout effect across 1246 cancer cell lines: 0.01 (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.