Chemokine CXC Receptors

Supporting information

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.

To view external sources of pharmacological information for Chemokine CXC Receptors, please click here: IUPHAR Receptor Code and BJP Guide

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
CXCR1 Human CXCR1 NM_000634 Q8N6T6
Mouse Cxcr1 NM_178241 Q810W6
Rat Cxcr1 NM_019310 P70612
CXCR2 Human CXCR2 NM_001557 P25025
Mouse Cxcr2 NM_009909 P35343
Rat Cxcr2 NM_017183 P35407
View all Chemokine CXC Receptor Gene Data »

Literature for Chemokine CXC Receptors

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GPCR Product Listing
Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

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  • Chemotaxis
  • Complement System
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Immunology Product Listing
Angiogenesis Life Science Poster

Written by Yongping Crawford and Napoleone Ferrara, this poster highlights major targets for antiangiogenic therapy, namely tumor- and stromal cell-derived pathways. Intrinsic and acquired resistance are described; antiangiogenic therapies targeting the VEGF pathway are also summarized. Compounds available from Tocris are listed.

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Angiogenesis Life Science Poster

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Cancer Research Product Guide

Cancer Research Product Guide

Our Cancer Research Guide highlights over 750 products for cancer research. Request copy or view PDF today.

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Immunology Guide

Immunology Product Listing

Our Immunology listing highlights over 190 products for immunology research. Request copy or view PDF today.

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GPCR Product Listing

GPCR Product Listing

Highlights over 450 products for GPCRs Request copy or view PDF today.

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VEGF Pathway & Anti-Angiogenic Therapy

Written by N. Ferrara & Y. Crawford

Angiogenesis Life Science Poster

A summary of antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance. Request copy today.

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