CXCR4 receptor

Chemokine receptor

C-X-C chemokine receptor type 4 (CXCR4) is a G protein-coupled receptor (GPCR) that specifically binds the chemokine CXCL12 (also known as stromal cell-derived factor-1 or SDF-1). CXCR4 is encoded by the CXCR4 gene located on chromosome 2 in humans.

Function

CXCR4 plays a crucial role in the immune system, particularly in the homing and migration of hematopoietic stem cells and leukocytes. It is also involved in the development of the cardiovascular system and the central nervous system. The receptor is implicated in various physiological and pathological processes, including cancer metastasis, HIV infection, and inflammatory diseases.

Mechanism of Action

Upon binding to its ligand CXCL12, CXCR4 activates downstream signaling pathways through the associated G proteins. This activation leads to various cellular responses, such as chemotaxis, cell survival, and proliferation. The receptor can also signal through β-arrestin-mediated pathways, which are involved in receptor desensitization and internalization.

Clinical Significance

CXCR4 is a co-receptor for HIV-1 entry into T cells, making it a target for antiretroviral therapies. In cancer, CXCR4 is often overexpressed and is associated with poor prognosis due to its role in promoting tumor growth and metastasis. Inhibitors of CXCR4, such as plerixafor, are used to mobilize hematopoietic stem cells for transplantation and are being investigated for their potential in cancer therapy.

Related Pages

• Chemokine
• G protein-coupled receptor
• Hematopoietic stem cell
• HIV
• Cancer metastasis
• Plerixafor

References

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