A2A/A2B adenosine receptor antagonist YZJ-5053

{
  "id": "MLC-T-ONC-009566",
  "term": "A2A/A2B adenosine receptor antagonist YZJ-5053",
  "field": "Oncology and biomedicine",
  "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.",
  "synonyms": [
    "A2AR/A2BR antagonist YZJ-5053",
    "adenosine receptor A2A/A2B antagonist YZJ-5053",
    "YZJ5053"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/a2a-a2b-adenosine-receptor-antagonist-yzj-5053/"
}