GCN2 inhibitor APL-4098
Term · Oncology and biomedicine · MLC-T-ONC-013912
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.
| Identifier | MLC-T-ONC-013912 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | general control nonderepressible 2 inhibitor APL-4098 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-013912",
"term": "GCN2 inhibitor APL-4098",
"field": "Oncology and biomedicine",
"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.",
"synonyms": [
"general control nonderepressible 2 inhibitor APL-4098"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/gcn2-inhibitor-apl-4098/"
}
Record 7,848 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.