Definition
C-X-C chemokine receptor type 4 (CXCR4) is a G-protein-coupled receptor (GPCR) for the chemoattractant cytokine (chemokine) CXCL12 (or stromal cell-derived factor-1alpha, SDF-1α). Along with the CC chemokine receptor 5 (CCR5), CXCR4 is a major coreceptor for the human immunodeficiency virus (HIV) on the surface of CD4+ cells. Attachment of the HIV envelope glycoprotein to CXCR4 allows for efficient fusion, entry, and replication of HIV (Su et al. 1999). Amino acid changes in the HIV gp120 glycoprotein, particularly in the V3 loop region, induce HIV to switch coreceptors from CCR5 to CXCR4 which is often associated to a late stage of disease progression or as a mechanism of virus resistance to drugs targeting CCR5. Drugs that block CXCR4 are potent inhibitors of CXCR4-using HIV strains in cell culture and in pilot drug efficacy studies. However, development of such agents has been halted due to adverse drug effects. The CXCR4 antagonist plerixafor (AMD3100, Mozobil®) has...
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Ballana, E., Esté, J.A. (2013). CXCR4, Coreceptors. In: Hope, T., Stevenson, M., Richman, D. (eds) Encyclopedia of AIDS. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-9610-6_81-1
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DOI: https://doi.org/10.1007/978-1-4614-9610-6_81-1
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