CXCR4 as a Radioligand Therapy Target
CXCR4, C-X-C motif chemokine receptor 4, is a cell-surface protein (GPCR). No tumor protein staining is recorded for it in Human Protein Atlas immunohistochemistry. Published literature reports that CXCR4 internalizes after ligand binding, which helps retain a radionuclide inside tumor cells. Clinical status: Clinical-stage (up to phase 3, any modality), with 1 active clinical trial.
Is CXCR4 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: No tumor staining in HPA immunohistochemistry.
- ✅ Internalization: Reported to internalize, which favors radionuclide retention.
- ✅ Clinical precedent: Clinical-stage (up to phase 3, any modality)
- ❔ Shedding: Not yet assessed.
- ❔ Normal-tissue dosimetry: Check kidney, liver, bone marrow and salivary expression in the Human Protein Atlas tissue atlas.
CXCR4 expression in cancer
No Human Protein Atlas tumor immunohistochemistry data is available for CXCR4.
Is CXCR4 internalized?
Yes. Agonists induced transient heteromerization coupled to receptor internalization.
Sources: PMID 42239782 · PMID 42125834 · PMID 41397322 · PMID 41330916 · PMID 41222235. AI-extracted from abstracts, so verify before citing.
CXCR4 clinical trials
Clinical-stage (up to phase 3, any modality). 1 active trial reference CXCR4 (ClinicalTrials.gov, accessed 2026-09-14).
CXCR4 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 CXCR4 in the Human Protein Atlas tissue atlas, and read how normal-tissue expression predicts radioligand dosimetry risk.
CXCR4 gene essentiality (DepMap)
CRISPR knockout effect across 1253 cancer cell lines: 0.04 (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.