Preferred Label : Rugocrixan;
NCIt synonyms : CX3CL1 Receptor Antagonist KAND567; CX3CR1 Antagonist AZD8797; CX3CR1 Antagonist KAND567; Fractalkine Receptor 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, rugocrixan 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. Rugocrixan 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.;
UNII : S9Y83SS7PQ;
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
