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Cancer Therapeutics
Egenix Translation Inhibition Platforms
Our first generation lead compounds, 4EGI-1 and 1181, block the activity of of eIF4E and eIF2α respectively, and have demonstrated potent activity against multiple cancer cell lines, anti-tumor activity in animal models, upregulation of apoptotic and tumor suppressor proteins, and downregulation of oncogenes including
- cyclin D1 – a protein involved in regulating the progression of cells through the cell cycle
- VEGF – Vascular Endothelial Growth Factor (which stimulates the growth of blood vessels)
- c-myc – a protein that binds to specific DNA sequences and controls the transcription of DNA to mRNA
with minimal adverse effects on “housekeeping” genes or basic cellular functions.
Inhibitors of translation initiation factor activity (eIF4E, Ternary Complex) selectively down regulate "weak" mRNAs and preferentially reduce expression of tumor promoting proteins and oncogenes. Translation of "housekeeping" genes ("strong" mRNAs) remain unaffected, which could translate into an advantageous safety profile.
