A Rhomboid in the Rough: Potent Inhibitors for a Previously Undruggable Target.

In this issue of Cell Chemical Biology, Tichá et al. (2017) report a novel class of highly potent and selective rhomboid inhibitors. Rhomboids are implicated in several devastating human afflictions including malaria, diabetes, cancer, and Parkinson's disease (PD), making them important drug targets for future therapeutics.