Chemokine CXC Receptors

Chemokine CXC receptors (CXCRs) predominantly recognize CXC chemokines. CXC chemokines are distinguished by having four conserved cysteines, with the first two cysteines being separated by a single amino acid. There are six chemokine CXC receptors, CXCR1 to 6, with each one having a distinct chemokine and leukocyte specificity.

CXCR1 and 2 are expressed on neutrophils and monocytes/macrophages, and are involved in acute inflammation and innate immunity. CXCR3 is expressed on circulating T cells, B cells and natural killer cells. CXCR4 is widely expressed on hematopoietic, vascular endothelial and neuronal cells, and is a coreceptor for HIV entry into CD4⁺ cells. Compounds targeting CXCR4, such as the antagonist AMD 3100, have been evaluated as potential therapies for HIV infection. This molecule has subsequently been developed as an immunostimulant and is used clinically to mobilize hematopoietic stem cells in patients undergoing autologous bone marrow transplantation for non-Hodgkin's lymphoma or multiple myeloma. CXCR5 is expressed in B-cells and Burkitt's lymphoma and is involved in B-cell migration into B-cell follicles and Peyer's patches. CXCR6 is expressed on activated T cells and T helper type 1 (Th1) and Th2 cells, which are important in inflammation.

A further chemokine receptor recognizing the CXC motif exists; it was previously known as CXCR7, but has been renamed ACKR3, or atypical chemokine receptor 3. ACKR3 mediates signaling via β-arrestin rather than G-proteins. It modulates the activity of CXCR4 by heterodimerizing with the receptor and scavenging CXCL12, the ligand for CXCR4. Upregulation of ACKR3 expression is associated with cancer growth and metastasis.

External sources of pharmacological information for Chemokine CXC Receptors :

• IUPHAR Receptor Code

• BJP Guide

Literature for Chemokine CXC Receptors

Tocris offers the following scientific literature for Chemokine CXC Receptors to showcase our products. We invite you to request* your copy today!

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Rheumatoid Arthritis Poster

Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.

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Chemokine CXC Receptor Gene Data