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- NCIT_C179629 IAO_0000115 "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)." @default.
- NCIT_C179629 NCIT_A7 NCIT_C38612 @default.
- NCIT_C179629 NCIT_NHC0 "C179629" @default.
- NCIT_C179629 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C179629 NCIT_P108 "A2AR Antagonist EXS21546" @default.
- NCIT_C179629 NCIT_P208 "CL1662148" @default.
- NCIT_C179629 NCIT_P322 "GDC" @default.
- NCIT_C179629 NCIT_P399 "804838" @default.
- NCIT_C179629 normalizedInformationContent "100" @default.
- NCIT_C179629 referenceCount "1" @default.
- NCIT_C179629 hasExactSynonym "A2AR Antagonist EXS21546" @default.
- NCIT_C179629 hasExactSynonym "EXS 21546" @default.
- NCIT_C179629 hasExactSynonym "EXS-21546" @default.
- NCIT_C179629 hasExactSynonym "EXS21546" @default.
- NCIT_C179629 inSubset NCIT_C128784 @default.
- NCIT_C179629 inSubset NCIT_C157711 @default.
- NCIT_C179629 inSubset NCIT_C157712 @default.
- NCIT_C179629 inSubset NCIT_C176424 @default.
- NCIT_C179629 type Class @default.
- NCIT_C179629 isDefinedBy ncit.owl @default.
- NCIT_C179629 label "A2AR Antagonist EXS21546" @default.
- NCIT_C179629 subClassOf NCIT_C179629 @default.
- NCIT_C179629 subClassOf NCIT_C1908 @default.
- NCIT_C179629 subClassOf NCIT_C1909 @default.
- NCIT_C179629 subClassOf NCIT_C201170 @default.
- NCIT_C179629 subClassOf NCIT_C2139 @default.
- NCIT_C179629 subClassOf NCIT_C308 @default.