Preferred Label : GCN2 Inhibitor APL-4098;
NCIt synonyms : General Control Nonderepressible 2 Inhibitor APL-4098;
NCIt definition : An orally bioavailable inhibitor of the serine/threonine protein kinase general control
nonderepressible 2 (GCN2; eukaryotic translation initiation factor 2-alpha kinase
4; GCN2 EIF2alpha kinase; eIF-2-alpha kinase GCN2), with potential antineoplastic
and immunomodulating activities. Upon oral administration, GCN2 inhibitor APL-4098
specifically targets, binds to and inhibits the activity of GCN2. This prevents GCN2-mediated
signaling and may induce apoptosis in tumor cells that rely on GCN2 signaling for
survival. In addition, as GCN2 signaling reduces anti-tumor immunity, preventing GCN2
signaling may enhance anti-tumor immune responses. GCN2 plays a key role in the activation
of the integrated stress response (ISR) pathway in response to amino acid deprivation
and in hypoxic tumors.;
Molecule name : APL 4098; APL-4098;
Origin ID : C212075;
concept_is_in_subset
- has_target
