ASGR1 as a Radioligand Therapy Target
ASGR1, asialoglycoprotein receptor 1, is a cell-surface protein (membrane receptor). In Human Protein Atlas immunohistochemistry, ASGR1 staining is highest in liver cancer (67% of samples positive), neuroendocrine tumors (75% of samples positive) and pancreatic cancer (17% of samples positive). Evidence on whether ASGR1 internalizes is mixed. Clinical status: Clinical-stage (up to phase 2, any modality).
Is ASGR1 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 liver cancer, 67% 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.
ASGR1 expression in cancer
Protein expression of ASGR1 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 |
|---|---|---|---|
| Liver Cancer | 0.64 | High | 67% |
| Neuroendocrine Tumors | 0.33 | Medium | 75% |
| Pancreatic Cancer | 0.11 | Low | 17% |
Not detected by IHC in: skin cancer, colorectal cancer, head and neck cancer, ovarian cancer, lymphoma, breast cancer, melanoma, kidney cancer, thyroid cancer, bladder cancer, cervical cancer, lung cancer, prostate cancer, gastric cancer, testicular cancer, endometrial cancer, glioma.
Is ASGR1 internalized?
Uncertain. Insufficient literature found.
ASGR1 clinical trials
Clinical-stage (up to phase 2, any modality). Nuclens hasn't indexed trials for ASGR1 yet. Search ClinicalTrials.gov for ASGR1 trials.
ASGR1 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 ASGR1 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
ASGR1 gene essentiality (DepMap)
CRISPR knockout effect across 1257 cancer cell lines: 0.07 (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 liver cancer radioligand targets
EGFR · c-MET (MET) · HER3 (ERBB3) · SSTR2 · STEAP2 · HER2 (ERBB2) · Mesothelin (MSLN) · B7-H3 (CD276)
See all radioligand therapy targets in liver 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.