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- Be563249cbf710cedc5f775f2ef5cc3d2 NCIT_P378 "NCI" @default.
- Be563249cbf710cedc5f775f2ef5cc3d2 type Axiom @default.
- Be563249cbf710cedc5f775f2ef5cc3d2 annotatedProperty IAO_0000115 @default.
- Be563249cbf710cedc5f775f2ef5cc3d2 annotatedSource NCIT_C170952 @default.
- Be563249cbf710cedc5f775f2ef5cc3d2 annotatedTarget "An orally bioavailable inhibitor of the ectoenzyme CD73 (cluster of differentiation 73; 5'-ecto-nucleotidase; 5'-NT; ecto-5'-nucleotidase), with potential immunomodulating and antineoplastic activities. Upon oral administration, CD73 inhibitor LY3475070 targets and binds to CD73, leading to clustering of and internalization of CD73. This prevents CD73-mediated conversion of adenosine monophosphate (AMP) to adenosine and decreases the amount of free adenosine in the tumor microenvironment (TME). This prevents adenosine-mediated lymphocyte suppression and increases the activity of CD8-positive effector cells and natural killer (NK) cells. This also activates macrophages and reduces the activity of myeloid-derived suppressor cells (MDSCs) and regulatory T-lymphocytes (Tregs). By abrogating the inhibitory effect on the immune system and enhancing the cytotoxic T-cell-mediated immune response against tumor cells, tumor cell growth decreases. In addition, clustering and internalization of CD73 decreases the migration of cancer cells and prevents metastasis. CD73, a plasma membrane protein belonging to the 5'-nucleotidase (NTase) family, catalyzes the conversion of extracellular nucleotides, such as AMP, to membrane-permeable nucleosides, such as adenosine. It is upregulated in a number of cancer cell types and plays a key role in adenosine-mediated immunosuppression within the TME." @default.