Preferred Label : Adenosine A2A Receptor Antagonist CS3005;
NCIt synonyms : A2AR Antagonist CS3005;
NCIt definition : An orally bioavailable immune checkpoint inhibitor and antagonist of the adenosine
A2A receptor (A2AR; ADORA2A), with potential immunomodulating and antineoplastic activities.
Upon administration, A2AR antagonist CS3005 selectively binds to and inhibits A2AR
expressed on T-lymphocytes. This prevents tumor-released adenosine from interacting
with the A2A receptors, thereby blocking the adenosine/A2AR-mediated inhibition of
T-lymphocytes. This results in the proliferation and activation of T-lymphocytes,
and stimulates a T-cell-mediated immune response against tumor cells. A2AR, a G protein-coupled
receptor, is highly expressed on the cell surfaces of T-cells and, upon activation
by adenosine, inhibits their proliferation and activation. Adenosine is often overproduced
by cancer cells and plays a key role in immunosuppression.;
Molecule name : CS-3005; CS 3005;
NCI Metathesaurus CUI : CL1412853;
Origin ID : C175468;
UMLS CUI : C5446549;
Semantic type(s)
concept_is_in_subset