General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases (Cell Chemical Biology)

Ticha et al. discover rhomboid protease inhibitors that are unprecedentedly potent and selective. They are based on a pharmacologically compliant chemotype and can thus serve as hitherto unavailable specific tools for cell biology or can yield lead compounds targeting rhomboids in medically relevant contexts such as malaria or Parkinson`s disease.