Preferred Label : CD73 Inhibitor ATG-037;
NCIt synonyms : CD73 Inhibitor CB-708;
NCIt definition : 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.;
Molecule name : ATG 037; CB 708; CB-708; ATG-037;
NCI Metathesaurus CUI : CL1778792;
Origin ID : C186654;
UMLS CUI : C5667070;
Semantic type(s)
- concept_is_in_subset
- has_target
