Preferred Label : DGK Alpha/Zeta Inhibitor BMS-986408;
NCIt synonyms : Diacylglycerol Kinase Inhibitor BMS-986408; DGK-alpha/zeta Inhibitor BMS-986408; DGK Inhibitor BMS-986408; DGKa/z Inhibitor BMS-986408;
NCIt definition : An orally bioavailable inhibitor of both the alpha-isoenzyme of diacylglycerol kinase
(DGK-alpha; DGKa) and the zeta-isoenzyme DGK-zeta (DGKz), with potential immune checkpoint
inhibitory and antineoplastic activities. Upon oral administration, DGK alpha/zeta
inhibitor BMS-986408 targets, binds to and blocks both DGKa and DGKz 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. In addition,
inhibition of DGKa and DGKz, overexpressed on certain tumor cells, may induce apoptosis
and inhibit proliferation. DGKa and DGKz are involved in the negative regulation of
second messenger signaling through lipid phosphorylation. Highly expressed in T-lymphocytes,
DGKa and DGKz regulate TCR signaling, promote T-cell anergy, and play a key role in
the downregulating of T-cell responses in tumors. DGKa and DGKz, also highly expressed
in various cancers, promote cancer cell survival through its anti-apoptosis and pro-proliferation
activities.;
Molecule name : BMS-986408; BMS 986408;
Origin ID : C211877;
concept_is_in_subset
- has_target
