Preferred Label : DGK-alpha Inhibitor GS-9911;
NCIt synonyms : DGKa Inhibitor GS-9911;
NCIt definition : An orally bioavailable inhibitor of the alpha-isoenzyme of diacylglycerol kinase (DGK-alpha;
DGKa), with potential immune checkpoint inhibitory and antineoplastic activities.
Upon oral administration, DGKa inhibitor GS-9911 targets, binds to and blocks DGKa
expressed on T-cells, thereby preventing the conversion of diacylglycerol (DAG) to
phosphatidic acid (PA). This induces DAG-mediated T-cell receptor (TCR)-mediated T-cell
signaling, induces T-cell proliferation, restores T-cell function, enhances cytokine
production, and activates a cytotoxic T-cell-mediated anti-tumor immune response.
This induces apoptosis and suppresses proliferation of susceptible tumor cells. DGKa
is involved in the negative regulation of second messenger signaling through lipid
phosphorylation. DGKa is highly expressed in various cancers and promotes cancer cell
survival through its anti-apoptosis and pro-proliferation activities. Also highly
expressed in T-lymphocytes, DGKa regulates TCR signaling, promotes T-cell anergy,
and plays a key role in the downregulating of T-cell responses in tumors.;
Molecule name : GS-9911; GS 9911;
NCI Metathesaurus CUI : CL1921226;
Origin ID : C202238;
UMLS CUI : C5907959;
Semantic type(s)
- concept_is_in_subset
- has_target
