Preferred Label : Adenosine Receptor A2A/A2B Antagonist M1069;
NCIt synonyms : A2A/A2B Adenosine Receptor Antagonist M1069; Dual Adenosine Receptor Antagonist M1069; A2AR/A2BR Antagonist M1069;
NCIt definition : 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.;
Molecule name : M-1069; M 1069;
NCI Metathesaurus CUI : CL1779172;
Origin ID : C186671;
UMLS CUI : C5667080;
Semantic type(s)
- concept_is_in_subset
