Product Feature - Chemokine Receptors

Chemokines (chemotactic cytokines) belong to a family of chemoattractant molecules involved in the directed migration of immune cells. Over fifty human chemokines have been identified that can be categorised into four groups: CC, CXC, CX3C and C (XCL1 and XCL2), depending on the spacing of their first two cysteine residues. Chemokines exert their effects by binding to G-protein-coupled chemokine receptors on the surface of cells, predominantly leukocytes. Eighteen human chemokine receptors have been identified that are classified according to the class of chemokines that they bind.

Key chemokine receptor compounds now available from Tocris include:

Potent CCR1 antagonist
J 113863
Improves paw inflammation, joint damage and dramatically reduces cell infiltration into joints in collagen-induced arthritis in mice.

Highly selective CCR2 antagonist
RS 504393
Inhibits MCP-1 chemotaxis (IC₅₀ = 330 nM) and ischaemia-reperfusion injury in kidneys.

Selective CCR1 antagonist
BX 513
Inhibits MIP-1α-induced intracellular calcium mobilisation (IC₅₀ = 2.5 μM). Also a full inverse agonist at US28, a HCMV-encoded chemokine receptor.

Potent and selective CXCR2 antagonist
SB 225002
Inhibits CINC-induced chemotaxis and attenuates neutrophil accumulation in inflammatory lung injury in vivo.

View all Chemokine Related Products.

Chemokine Function

The major function of chemokines is to regulate leukocyte trafficking in haematopoiesis and in innate and adaptive immunity. Other functions include angiogenic activity, apoptosis, T-cell differentiation and phagocyte activation. Inadvertent activation of chemokine receptors leads to autoimmunity by inappropriately targeting self antigens for destruction by cytotoxic T-cells and macrophages.

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