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- NCIT_C186671 IAO_0000115 "An orally bioavailable antagonist of both the immunomodulatory checkpoint molecules adenosine A2A receptor (A2AR; ADORA2A) and A2B receptor (A2BR; ADORA2B), with potential immunomodulating and antineoplastic activities. Upon oral administration, adenosine A2A/A2B receptor antagonist M1069 competes with tumor-released adenosine for binding to A2AR and A2BR expressed on numerous intratumoral immune cells, such as dendritic cells (DCs), natural killer (NK) cells, macrophages and T-lymphocytes. The binding of M1069 to A2AR and A2BR inhibits A2AR/A2BR activity and prevents adenosine-A2AR/A2BR-mediated signaling. A2AR/A2BR inhibition activates and enhances the proliferation of various immune cells, abrogates the adenosine-mediated immunosuppression in the tumor microenvironment (TME) and activates the immune system to exert anti-tumor immune responses against cancer cells, which leads to tumor cell killing. A2AR and A2BR, G protein-coupled signaling receptors, are expressed on the cell surfaces of numerous immune cells. Adenosine is often overproduced by tumor cells and plays a key role in immunosuppression and tumor cell proliferation." @default.
- NCIT_C186671 NCIT_NHC0 "C186671" @default.
- NCIT_C186671 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C186671 NCIT_P108 "Adenosine Receptor A2A/A2B Antagonist M1069" @default.
- NCIT_C186671 NCIT_P208 "CL1779172" @default.
- NCIT_C186671 NCIT_P322 "GDC" @default.
- NCIT_C186671 NCIT_P399 "809142" @default.
- NCIT_C186671 normalizedInformationContent "100" @default.
- NCIT_C186671 referenceCount "1" @default.
- NCIT_C186671 hasExactSynonym "A2A/A2B Adenosine Receptor Antagonist M1069" @default.
- NCIT_C186671 hasExactSynonym "A2AR/A2BR Antagonist M1069" @default.
- NCIT_C186671 hasExactSynonym "Adenosine Receptor A2A/A2B Antagonist M1069" @default.
- NCIT_C186671 hasExactSynonym "Dual Adenosine Receptor Antagonist M1069" @default.
- NCIT_C186671 hasExactSynonym "M 1069" @default.
- NCIT_C186671 hasExactSynonym "M-1069" @default.
- NCIT_C186671 hasExactSynonym "M1069" @default.
- NCIT_C186671 inSubset NCIT_C128784 @default.
- NCIT_C186671 inSubset NCIT_C157711 @default.
- NCIT_C186671 inSubset NCIT_C157712 @default.
- NCIT_C186671 inSubset NCIT_C176424 @default.
- NCIT_C186671 type Class @default.
- NCIT_C186671 isDefinedBy ncit.owl @default.
- NCIT_C186671 label "Adenosine Receptor A2A/A2B Antagonist M1069" @default.
- NCIT_C186671 subClassOf NCIT_C186671 @default.
- NCIT_C186671 subClassOf NCIT_C1908 @default.
- NCIT_C186671 subClassOf NCIT_C1909 @default.
- NCIT_C186671 subClassOf NCIT_C201170 @default.
- NCIT_C186671 subClassOf NCIT_C201171 @default.
- NCIT_C186671 subClassOf NCIT_C2139 @default.
- NCIT_C186671 subClassOf NCIT_C308 @default.