Figure 3: Targeting pluripotency factors to inhibit breast cancer progression.
The small molecule inhibitor 8866 inhibits MYC-driven human breast tumors via blockade of IRE1-mediated activation of the cMYC/XBP1 transcriptional complex. Targeting activation of E3 ubiquitin ligase Carboxy Terminus of HSP70-Interacting Protein (CHIP) could lead to increased degradation of the breast CSC-associated factor OCT4. Inhibiting phosphorylation of threonine 116 on SOX2 could prevent SOX2-mediated transcription and promotion of CSC-related genes. The AKT inhibitor, MK2206 prevents phosphorylation-mediated translocation of SOX2 to the nucleus to activate target genes involved in breast cancer proliferation and stemness.