CXCR4
A chemokine receptor that anchors blood cells in the marrow and helps cancer cells home to it; mutated in a third of Waldenström patients and targeted by plerixafor for stem-cell mobilisation.
CXCR4 binds CXCL12 (SDF-1) to retain haematopoietic stem cells in the marrow niche and guides metastasis of solid tumours to bone. Plerixafor (2008) blocks it to mobilise stem cells for autologous transplant; motixafortide (2023) does the same in myeloma. WHIM-like CXCR4 mutations in ~30-40% of Waldenström macroglobulinaemia slow BTK-inhibitor response; mavorixafor is in trials. CXCR4 is also imaged with Ga-68 pentixafor and treated with Lu-177 pentixather in marginal zone lymphoma and myeloma (theranostic, experimental). Balixafortide and ulocuplumab failed in solid tumours.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · A chemokine receptor that anchors blood cells in the marrow and helps cancer cells home to it; mutated in a third of Waldenström patients and targeted by plerixafor for stem-cell mobilisation.
- 1 · What it is
A chemokine receptor that anchors blood cells in the marrow and helps cancer cells home to it; mutated in a third of Waldenström patients and targeted by plerixafor for stem-cell mobilisation.
- 2 · What goes wrong in cancer
G-protein-coupled receptor; CXCL12 binding activates Gαi, PI3K/AKT and MAPK, promoting chemotaxis, survival and retention in stromal niches; truncating C-terminal mutations impair receptor internalisation (WHIM syndrome).
- 3 · How drugs use it
No product in this corpus aims at CXCR4 yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
Biology
G-protein-coupled receptor; CXCL12 binding activates Gαi, PI3K/AKT and MAPK, promoting chemotaxis, survival and retention in stromal niches; truncating C-terminal mutations impair receptor internalisation (WHIM syndrome).
- Waldenström macroglobulinaemia (30-40% mutation)
- Myeloma, lymphoma, AML (expression)
- Breast, prostate and other solid tumours (metastatic homing)
How common it is, by cancer
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Waldenström macroglobulinaemia | 30-40% | CXCR4 mutation | doi.org |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Latest papers
topQuery for this target: (TITLE:"CXCR4" OR ABSTRACT:"CXCR4") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about CXCR4, not a curated reading list.
Pages like this
not linked directly; found by shared links- TargetCSF1R
Shares The pre-metastatic niche, Myeloid suppression: TAMs, MDSCs & don't-eat-me signals, Cold tumours: immune deserts and exclusion and the tag gap-fill.
- ProductPexidartinib
Shares Myeloid suppression: TAMs, MDSCs & don't-eat-me signals and the tag gap-fill.
- ProductPanobinostat
Shares Multiple myeloma and the tag gap-fill.
- TargetVISTA
Shares Myeloid suppression: TAMs, MDSCs & don't-eat-me signals and the tag gap-fill.
- ProductTazemetostat
Shares Cold tumours: immune deserts and exclusion and the tag gap-fill.
- ProductElotuzumab
Shares Multiple myeloma and the tag gap-fill.
- ProductGlasdegib
Shares Acute myeloid leukaemia and the tag gap-fill.
- TargetCD7
Shares Acute myeloid leukaemia and the tag gap-fill.