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.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
5795 ATI 2341
CXCR4 allosteric agonist
4780 VUF 11207 fumarate
Potent ACKR3 (CXCR7) agonist
5668 VUF 11222
High affinity non-peptide CXCR3 agonist

Antagonists

Cat No Product Name / Activity
3299 AMD 3100 octahydrochloride
Highly selective CXCR4 antagonist
4179 AMD 3465 hexahydrobromide
Potent and selective CXCR4 antagonist
4487 (±)-AMG 487
CXCR3 antagonist; inhibits cell migration and metastasis
5872 AZ 10397767
Potent CXCR2 antagonist
5130 CTCE 9908
CXCR4 antagonist; antitumor
4320 FC 131
CXCR4 antagonist
4596 IT1t dihydrochloride
Potent CXCR4 antagonist
5943 ML 339
Potent and selective hCXCR6 antagonist
4528 (±)-NBI 74330
Potent and selective CXCR3 antagonist
5660 NVP CXCR2 20
Potent and selective CXCR2 antagonist
2725 SB 225002
Potent and selective CXCR2 antagonist
2724 SB 265610
Potent CXCR2 antagonist
5671 SB 332235
Potent CXCR2 antagonist
4300 TC 14012
CXCR4 antagonist; ACKR3 (CXCR7) agonist
3951 WZ 811
Potent CXCR2 antagonist

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 :

Literature for Chemokine CXC Receptors

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Immunology

Immunology Product Listing

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

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation

Chemokine CXC Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
CXCR1 Human CXCR1 NM_000634 P25024
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
CXCR3 Human CXCR3 NM_001142797 P49682
Mouse Cxcr3 NM_009910 O88410
Rat Cxcr3 NM_053415 Q9JII9
CXCR4 Human CXCR4 NM_001008540 P61073
Mouse Cxcr4 NM_009911 P70658
Rat Cxcr4 NM_022205 O08565
CXCR5 Human CXCR5 NM_001716 P32302
Mouse Cxcr5 NM_007551 Q04683
Rat Cxcr5 NM_053303 P34997
CXCR6 Human CXCR6 NM_006564 O00574
Mouse Cxcr6 NM_030712 Q9EQ16
Rat Cxcr6 NM_001102587 NP_001096057
ACKR3 Human ACKR3 NM_020311 P25106
Mouse Ackr3 NM_001271607 P56485
Rat Ackr3 NM_053352 O89039