# CXCR4

Source: https://nuclide.cc/targets/cxcr4/  
Nuclide record `cxcr4` (Target). Data CC BY-NC 4.0, attribute "Data from Nuclide (nuclide.cc)"; commercial use needs a licence.

## TL;DR

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.

## Summary

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.

## Fields

- Kind: Target
- Last checked: 2026-09-08
- Tags: gap-fill
- Symbol: CXCR4
- Class: other
- 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).
- Where found: Waldenström macroglobulinaemia (30-40% mutation); Myeloma, lymphoma, AML (expression); Breast, prostate and other solid tumours (metastatic homing)

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/CXCR4
- CXCR4 in WM (Blood 2014): https://doi.org/10.1182/blood-2014-01-550905

## Connected records

- isotopes: [Gallium-68](https://nuclide.cc/isotopes/ga-68/), [Lutetium-177](https://nuclide.cc/isotopes/lu-177/)
- technologies: [Radioligand therapy (beta emitters)](https://nuclide.cc/technologies/radioligand-therapy/)
- terms: [Theranostics](https://nuclide.cc/terms/theranostics/)
- indications: [Primary aldosteronism](https://nuclide.cc/indications/primary-aldosteronism/)
- opportunities: [CXCR4 imaging instead of adrenal vein sampling](https://nuclide.cc/opportunities/opp-cxcr4-primary-aldosteronism/)
- drugs: [Gallium-68 pentixafor](https://nuclide.cc/drugs/ga-68-pentixafor/)

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