Preferred Label : CD73 Inhibitor LY3475070;
NCIt related terms : LY-3475070;
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 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.;
UNII : AKA9175T4N;
Molecule name : LY-3475070; LY 3475070;
NCI Metathesaurus CUI : CL1383223;
Origin ID : C170952;
UMLS CUI : C5417838;
- Semantic type(s)
- concept_is_in_subset
- has_target