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Items: 3

1.

Adenosine-A2A Receptor Antagonist CPI-444

A small molecule immune checkpoint inhibitor of the adenosine A2A receptor (ADORA2A) with potential antineoplastic activity. Upon oral administration, adenosine-A2A receptor antagonist CPI-444 binds to adenosine A2A receptors expressed on the surface of immune cells, including T-lymphocytes, natural killer (NK) cells, macrophages and dendritic cells (DCs). This prevents tumor-released adenosine from interacting with the A2A receptors on these key immune surveillance cells, thereby abrogating adenosine-induced immunosuppression in the tumor microenvironment. This may stimulate anti-tumor immune responses, resulting in tumor regression. [from NCI]

MedGen UID:
903219
Concept ID:
C4085936
Immunologic Factor; Pharmacologic Substance
2.

Deficiency of adenosine kinase

MedGen UID:
713685
Concept ID:
C1291378
Disease or Syndrome
3.

Acadesine

A 5-aminoimidazole-4-carboxamide (AICA) riboside, a ribnucleoside analog, and a nucleotide biosynthesis precursor with B cell pro-apoptotic activity. Following cellular uptake, acadesine is phosphorylated to AICA ribotide (ZMP), which mimics 5'-adenosine monophosphate (AMP). Both AMP-activated protein kinase (AMPK) and AMPK kinase (AMPKK) are activated by ZMP, which appears to be necessary for the induction of apoptosis. Acadesine-induced apoptosis also appears to require cytochrome c release from mitochondria and caspase activation and is p53-independent. However, the exact mechanism of acadesine-induced apoptosis is unknown. T cells are significantly less susceptible than B cells to acadesine-induced apoptosis. AMPK regulates several cellular systems including the cellular uptake of glucose, the beta-oxidation of fatty acids, protein synthesis, and the biogenesis of glucose transporter 4 (GLUT4) and mitochondria. [from NCI]

MedGen UID:
62345
Concept ID:
C0051027
Nucleic Acid, Nucleoside, or Nucleotide; Pharmacologic Substance
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