CX3C chemokine receptor 1 (CX3CR1) (CX3CR1)

CX3C chemokine receptor 1 (CX3CR1) is a G protein-coupled receptor primarily expressed on microglia, monocytes, and natural killer cells (UniProt P49238). It serves as the unique receptor for the chemokine CX3CL1 (fractalkine), which is expressed by neurons and endothelial cells. The CX3CL1/CX3CR1 axis is a critical communication pathway that regulates the migration, adhesion, and polarization of microglia and macrophages. In the central nervous system, this axis maintains microglia in a homeostatic state; however, its dysregulation is linked to neurodegenerative diseases like Alzheimer's and Parkinson's, where it influences the shift between pro-inflammatory (M1-like) and anti-inflammatory (M2-like) phenotypes (PMID: 30655347). Pharmacological targeting of CX3CR1, primarily through small molecule antagonists like KAND567, is being investigated to reduce chronic inflammation and tissue damage in conditions such as atherosclerosis, neuropathic pain, and various inflammatory disorders (Kancera AB).

Other names

Fractalkine receptorG-protein coupled receptor 13GPR13V28CMKBRL1

Antagonism of the CX3CR1 receptor to inhibit the recruitment of inflammatory cells and modulate the polarization of microglia and macrophages from pro-inflammatory to anti-inflammatory states (PMID: 30655347).