NXP800 MOA

NXP800 is an orally bioavailable small molecule activator of the GCN2 kinase.
GCN2 phosphorylates the eukaryotic translation initiation factor 2 (eIF2), which results in lower bulk protein synthesis and in induction of preferential translation of stress-adaptive gene transcripts, such as that encoding the ATF4 transcription regulator. Chronic activation of GCN2 by NXP800 leads to cancer cell death.

Abbreviations: ATF4 = activating transcription factor 4; CHOP = CCAAT (cytosine-cytosine-adenosine-adenodine-thymidine)-enhancer-binding protein homologous protein; eIF2α = eukaryotic initiation factor 2 alpha;
GCN2 = general control nonderepressible 2; PD = pharmacodynamic; tRNA = transfer ribonucleic acid.