title: Rhomboid protease inhibitors: Emerging tools and future therapeutics.
abstract: Rhomboid-family intramembrane serine proteases are evolutionarily widespread. Their functions in different organisms are gradually being uncovered and already suggest medical relevance for infectious diseases and cancer. In contrast to these advances, selective inhibitors that could serve as efficient tools for investigation of physiological functions of rhomboids, validation of their disease relevance or as templates for drug development are lacking. In this review I extract what is known about rhomboid protease mechanism and specificity, examine the currently used inhibitors, their mechanism of action and limitations, and conclude by proposing routes for future development of rhomboid protease inhibitors.
authors: Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Flemingovo n. 2, Prague 166 10, Czech Republic. Electronic address: kvido.strisovsky@uochb.cas.cz.
authors: Kvido
authors: K
authors: Strisovsky
mesh_terms: D000818:Animals; D057075:Enzyme Assays; D006801:Humans; D008565:Membrane Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D058990:Molecular Targeted Therapy; D011480:Protease Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D008565:Membrane Proteins; D011480:Protease Inhibitors
keywords: Disease; Inhibitor; Mechanism; Rhomboid protease; Substrate specificity