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- NCIT_C186654 IAO_0000115 "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 ATG-037 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.
- NCIT_C186654 NCIT_A7 NCIT_C114927 @default.
- NCIT_C186654 NCIT_NHC0 "C186654" @default.
- NCIT_C186654 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C186654 NCIT_P108 "CD73 Inhibitor ATG-037" @default.
- NCIT_C186654 NCIT_P208 "CL1778792" @default.
- NCIT_C186654 NCIT_P322 "GDC" @default.
- NCIT_C186654 NCIT_P399 "809158" @default.
- NCIT_C186654 normalizedInformationContent "100" @default.
- NCIT_C186654 referenceCount "1" @default.
- NCIT_C186654 hasExactSynonym "ATG 037" @default.
- NCIT_C186654 hasExactSynonym "ATG-037" @default.
- NCIT_C186654 hasExactSynonym "ATG037" @default.
- NCIT_C186654 hasExactSynonym "CB 708" @default.
- NCIT_C186654 hasExactSynonym "CB-708" @default.
- NCIT_C186654 hasExactSynonym "CB708" @default.
- NCIT_C186654 hasExactSynonym "CD73 Inhibitor ATG-037" @default.
- NCIT_C186654 hasExactSynonym "CD73 Inhibitor CB-708" @default.
- NCIT_C186654 inSubset NCIT_C128784 @default.
- NCIT_C186654 inSubset NCIT_C157711 @default.
- NCIT_C186654 inSubset NCIT_C157712 @default.
- NCIT_C186654 inSubset NCIT_C176424 @default.
- NCIT_C186654 type Class @default.
- NCIT_C186654 isDefinedBy ncit.owl @default.
- NCIT_C186654 label "CD73 Inhibitor ATG-037" @default.
- NCIT_C186654 subClassOf NCIT_C129820 @default.
- NCIT_C186654 subClassOf NCIT_C186654 @default.
- NCIT_C186654 subClassOf NCIT_C1908 @default.
- NCIT_C186654 subClassOf NCIT_C1909 @default.
- NCIT_C186654 subClassOf NCIT_C274 @default.
- NCIT_C186654 subClassOf NCIT_C308 @default.