title: Mechanism and Inhibition of Rhomboid Proteases.
abstract: Intramembrane serine proteases of the rhomboid family are widespread, and their gradually uncovered functions in different organisms already suggest medical relevance for infectious diseases and cancer. However, selective inhibitors that could serve as research tools for rhomboids, for validation of their disease relevance, or as templates for drug development are lacking. Here I summarize the current knowledge about rhomboid protease mechanism and specificity, overview the currently used inhibitors, and conclude by proposing avenues for future development of rhomboid protease inhibitors.
authors.affiliation: Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Prague, Czech Republic. Electronic address: kvido.strisovsky@uochb.cas.cz.
authors.forename: K
authors.initials: K
authors.lastname: Strisovsky
mesh_terms: D010450:Endopeptidases / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D008565:Membrane Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry*; D011480:Protease Inhibitors / Q000737:chemistry; D013379:Substrate Specificity
chemical_list: D008565:Membrane Proteins; D011480:Protease Inhibitors; D010450:Endopeptidases
keywords: Disease; Inhibitor; Mechanism; Rhomboid protease; Substrate specificity