Chemokine

The CCR1 receptor is a member of the beta chemokine receptor family (GPCR-A1). Chemokines and their receptors are critical for the recruitment of effector immune cells to the site of inflammation. The ligands of this receptor include macrophage inflammatory protein 1 alpha (MIP-1 alpha), regulated on activation normal T expressed and secreted protein (RANTES), monocyte chemoattractant protein 3 (MCP-3), and myeloid progenitor inhibitory factor-1 (MPIF-1). Following interaction with their specific chemokine ligands, chemokine receptors trigger a flux in intracellular calcium (Ca2+) ions (calcium signaling). This causes cell responses, including the onset of a process known as chemotaxis that traffics the cell to a desired location within the organism.
CXC chemokine receptors are integral membrane proteins (GPCR-A2) that specifically bind and respond to cytokines of the CXC chemokine family. CXCR1 and CXCR2 (IL8R-α and IL8R–β respectively) are closely related receptors that recognize CXC chemokines that possess an E-L-R amino acid motif immediately adjacent to their CXC motif; they are both expressed on the surface of neutrophils in mammals. While CXCR3 is expressed predominantly on < href="/products/research-areas/immunology">T lymphocytes, the CXCR4 receptor has a wide cellular distribution, with expression on most immature and mature <a " href="/products/research-areas/angiogenesis">hematopoietic cell types[1].
Fractalkine is a transmembrane protein and chemokine involved in the adhesion and migration of leukocytes. The protein encoded by this gene is a receptor for fractalkine (CX3CR1). CX3CR1 and its ligand help control the migration and recruitment of immune effector cells in numerous inflammatory diseases and may play a role in cancer progression, immune evasion, and metastasis. Increasing evidence indicates that CX3CR1 is required for monocyte homeostasis and differentiation and regulates the fate of monocyte-derived cells in other inflammatory diseases such as cardiovascular disease and liver fibrosis. However, precisely how CX3CR1 regulates tumor-associated macrophages (TAMs) subtypes in the tumor microenvironment remains unknown[2]. Besides, evidence is found that the fractalkine receptor also is a coreceptor for HIV-1, and some variations in this gene lead to increased susceptibility to HIV-1 infection and rapid progression to AIDS[3]


[1] Chemokine receptors and their role in inflammation and infectious diseases. Murdoch C., Finn A. Blood 2000, 95, 3032–3043
[2] J. Zheng et al. Chemokine receptor CX3CR1 contributes to macrophage survival in tumor metastasis. Mol. Cancer. 2013, 12, 141.
[3] R. Cotter et al. Fractalkine (CX3CL1) and brain inflammation: Implications for HIV-1-associated dementia. J. Neurovirol. 2002, 8, 585-598.

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Axon ID Name Description From price
1179 A1B1 hydrochloride CCR1 antagonist €125.00
1738 AMD 3100 CXCR4 antagonist €85.00
1930 AMD 3465 hexahydrobromide Potent and selective CXCR4 antagonist €85.00
2255 AZD 8797 Potent and selective antagonist of the Fractalkine receptor (FKN or CX3CR1) €120.00
2082 BX 471 Selective CCR1 receptor antagonist €105.00
2665 Cenicriviroc Oral CCR5-antagonist for treatment of HIV infection €145.00
1800 CXCR3 Antagonist 6c CXCR3 antagonist €145.00
1559 SB 265610 CXCR2 antagonist €95.00
2593 SB 332235 Nonpeptide CXCR2 antagonist exhibiting significant anti-inflammatory effects €105.00
2685 Vercirnon CCR9 antagonist €135.00
1620 WZ 811 CXCR4 antagonist €80.00
2636 YJC-10592 CCR2 antagonist €145.00

12 Item(s)

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