GCN2 Activator DCC-2812

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable activator of the serine/threonine protein kinase eIF-2-alpha kinase GCN2 (general control nonderepressible 2; eukaryotic translation initiation factor 2-alpha kinase 4), with potential antineoplastic activity. Upon oral administration, GCN2 activator DCC-2812 activates GCN2, which phosphorylates eukaryotic translation initiation factor 2A (eIF2A), thereby inducing cyclic AMP-dependent transcription factor ATF-4 transcription and ATF-4-mediated integrated stress response (ISR). This may result in apoptosis. GCN2 plays a key role in the activation of the ISR pathway in response to amino acid deprivation and in hypoxic tumors. While ISR promotes the adaptation of tumor cells to hypoxic stress, prolonged activation of ISR induces apoptosis.

**Synonyms:** - DCC 2812 - DCC-2812 - DCC2812