" /> Etrumadenant - CISMeF





Preferred Label : Etrumadenant;

NCIt synonyms : A2AR/A2BR Antagonist AB928; Dual A2AR/A2BR Antagonist AB928; Adenosine A2A/A2B Receptor Antagonist AB928;

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 administration, etrumadenant 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 AB928 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.;

UNII : W0ZE0NT8IF;

InChIKey : BUXIAWLTBSXYSW-UHFFFAOYSA-N;

CAS number : 2239273-34-6; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2239273-34-6 alt lien vers site G-SRS target _blank img src /img/logos/logo_g-srs.png alt Logo G-SRS /a ;

Molecule name : AB 928; AB-928;

NCI Metathesaurus CUI : CL951401;

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12/05/2024


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