Preferred Label : DGKalpha Inhibitor BAY 2862789;
NCIt synonyms : DGKa Inhibitor BAY 2862789; Diacylglycerol Kinase Alpha Inhibitor BAY 2862789;
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 BAY 2862789 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 antiapoptosis and proproliferation 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 : BAY 2862789; BAY-2862789;
NCI Metathesaurus CUI : CL1915100;
Origin ID : C200820;
UMLS CUI : C5854603;
Semantic type(s)
- concept_is_in_subset
- has_target
