Preferred Label : A2A/A2B Adenosine Receptor Antagonist YZJ-5053;
NCIt synonyms : A2AR/A2BR Antagonist YZJ-5053; Adenosine Receptor A2A/A2B Antagonist YZJ-5053; YZJ5053;
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, A2A/A2B
adenosine receptor antagonist YZJ-5053 competes with tumor-released adenosine for
binding to A2AR and A2BR expressed on numerous intra-tumoral immune cells, such as
dendritic cells (DCs), natural killer (NK) cells, macrophages and T-lymphocytes. The
binding of YZJ-5053 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 : YZJ-5053; SHY 1901; SHY-1901; YZJ 5053;
NCI Metathesaurus CUI : CL1928591;
Origin ID : C206257;
concept_is_in_subset
- has_target
