Preferred Label : A2AR Antagonist EXS21546;
NCIt definition : An orally bioavailable immune checkpoint inhibitor and antagonist of the adenosine
A2A receptor (A2AR; ADORA2A), with potential immunomodulating and antineoplastic activities.
Upon oral administration, A2AR antagonist EXS21546 selectively targets, 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 in the tumor microenvironment
(TME). EXS21546 does not penetrate the central nervous system (CNS).;
Molecule name : EXS-21546; EXS 21546;
NCI Metathesaurus CUI : CL1662148;
Origin ID : C179629;
UMLS CUI : C5555825;
Semantic type(s)
- concept_is_in_subset
- has_target
