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 T lymphocytes, the CXCR4 receptor has a wide cellular distribution, with expression on most immature and mature 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].
The CC chemokine receptor 8 (CCR8) belongs to the seven transmembrane-spanning receptor family and functionally responds to the eukaryotic CC chemokines I-309, thymus and activation-regulated chemokine, macrophage inflammatory protein-1 beta (MIP-1b) and to the products viral MIP-I and viral MIP-II of the Kaposi-associated herpesvirus (HHV-8).[4]
[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.
[4] M. Napolitano and A. Santoni. Structure and function of the CC chemokine receptor (CCR) 8. Forum (Genova). 1999 Oct-Dec;9(4):315-24.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
1179 | A1B1 hydrochloride | CCR1 antagonist | €125.00 | |
1738 | AMD 3100 | CXCR4 antagonist | €90.00 | |
1930 | AMD 3465 hexahydrobromide | Potent and selective CXCR4 antagonist | €85.00 | |
2842 | AZD2098 | Potent, selective and bioavailable CCR4 receptor antagonist | €125.00 | |
2255 | AZD8797 | 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 | €160.00 | |
1800 | CXCR3 Antagonist 6c | CXCR3 antagonist | €135.00 | |
2921 | LIT-927 | Selective, locally and orally active CXCL12 neutraligand | €95.00 | |
3774 | LN6023 dihydrochloride | First-in-class, selective ACKR3/CXCR7 superagonist | €150.00 | |
4167 | RS504393 | Selective CCR2 antagonist | €110.00 | |
1559 | SB 265610 | CXCR2 antagonist | €120.00 | |
2593 | SB 332235 | Nonpeptide CXCR2 antagonist exhibiting significant anti-inflammatory effects | €105.00 | |
2993 | UNBS5162 | Pan-antagonist of CXCL chemokine expression | €95.00 | |
2685 | Vercirnon | CCR9 antagonist | €135.00 | |
1620 | WZ 811 | CXCR4 antagonist | €80.00 | |
2636 | YJC-10592 | CCR2 antagonist | €145.00 | |
2861 | ZK 756326 dihydrochloride | CCR8 agonist | €90.00 |