Hitting Hsp90 where it hurts

Researchers at the University of Massachusetts Medical School have synthesized a class of targeted molecules called gamitrinibs that selectively inhibit Hsp90 in tumor mitochondria, the organelle where Hsp90 exerts many of its cancer-promoting effects. The compounds could have an advantage over the plethora of Hsp90 inhibitors in the clinic that exert their effects in the cytosol.¹

Heat shock protein 90 (HSP90AA1; Hsp90) is a chaperone that facilitates properprotein folding in multiple signaling pathways, including those that drive tumor development and progression. In tumor cell mitochondria, the protein can preserve organelle integrity and prevent the initiation of cell death.² By contrast, in most normal cells, Hsp90 is expressed in the cytosol, where it protects the cells from environmental stressors like heat and hypoxia...