Preferred Label : Fractalkine Receptor Antagonist KAND567;
NCIt synonyms : CX3CL1 Receptor Antagonist KAND567; CX3CR1 Antagonist AZD8797; CX3CR1 Antagonist KAND567;
NCIt definition : An orally bioavailable non-competitive and selective antagonist of the fractalkine
(C-X3-C motif chemokine 1; chemokine ligand 1; CX3CL1; small-inducible cytokine D1)
receptor (CX3C chemokine receptor 1; CX3CR1; chemokine, CX3C motif, receptor 1), with
potential anti-inflammatory, immunomodulatory and antineoplastic activities. Upon
oral administration, fractalkine receptor antagonist KAND567 specifically and allosterically
binds to and blocks CX3CR1, thereby preventing the binding of fractalkine to its receptor
and preventing the activity of CX3CR1. This prevents CX3CR1-mediated signaling, prevents
the recruitment and extravasation of CX3CR1-expressing subsets of leukocytes and monocytes
into tissues and vital organs and inhibits the exaggerated inflammatory response and
the associated tissue damage caused by hyperinflammation. KAND567 also binds to and
blocks CX3CR1 on cancer cells, thereby inhibiting proliferation of CX3CR1-expressing
tumor cells. In addition, blocking CX3CR1 may suppress DNA repair processes of damaged
DNA which prevents cancer cell survival following treatment with DNA damaging agents.
Fractalkine, an immunomodulating factor and chemokine, controls the function of certain
immune and cancer cells. Fractalkine and its receptor CX3CR1 are elevated in and play
key roles in several cancers, inflammatory diseases and heart disease.;
CAS number : 911715-90-7;
Molecule name : KAND-567; AZD 8797; KAND 567; AZD-8797;
NCI Metathesaurus CUI : CL1921211;
Origin ID : C202241;
UMLS CUI : C5907962;
Semantic type(s)
- concept_is_in_subset
- has_target
