Acridine Derivatives as Inhibitors of the IRE1α-XBP1 Pathway Are Cytotoxic to Human Multiple Myeloma.

@article{Jiang2016AcridineDA,
  title={Acridine Derivatives as Inhibitors of the IRE1α-XBP1 Pathway Are Cytotoxic to Human Multiple Myeloma.},
  author={Dadi Jiang and Arvin B. Tam and Muthuraman Alagappan and Michael P. Hay and A. Gupta and Margaret Manella Kozak and David E. Solow-Cordero and Pek Y. Lum and Nicholas C. Denko and Amato J. Giaccia and Quynh L{\^e} and Maho Niwa and Albert C. Koong},
  journal={Molecular cancer therapeutics},
  year={2016},
  volume={15 9},
  pages={2055-65}
}
Using a luciferase reporter-based high-throughput chemical library screen and topological data analysis, we identified N-acridine-9-yl-N',N'-dimethylpropane-1,3-diamine (DAPA) as an inhibitor of the inositol requiring kinase 1α (IRE1α)-X-box binding protein-1 (XBP1) pathway of the unfolded protein response. We designed a collection of analogues based on the… CONTINUE READING