Preferred Label : Quemliclustat;
NCIt synonyms : CD73 Inhibitor AB680;
NCIt definition : A small molecule, competitive inhibitor of the ectoenzyme CD73 (cluster of differentiation
73; 5'-ecto-nucleotidase; 5'-NT; ecto-5'-nucleotidase), with potential immunomodulating
and antineoplastic activities. Upon administration, quemliclustat 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 cancer 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, upregulated on a number of cancer cell types, catalyzes the conversion
of extracellular nucleotides, such as AMP, to membrane-permeable nucleosides, such
as adenosine; it plays a key role in adenosine-mediated immunosuppression within the
TME.;
UNII : J6K8WSV73A;
CAS number : 2105904-82-1; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2105904-82-1
alt lien vers site G-SRS target _blank img src /img/logos/logo_g-srs.png alt Logo
G-SRS /a ;
Molecule name : AB-680; AB 680;
NCI Metathesaurus CUI : CL972383;
Origin ID : C167156;
UMLS CUI : C5554572;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
