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Here, we report 4\u2010oxo\u2010\u03b2\u2010lactams as a novel scaffold for inhibition of rhomboids. We show that they covalently react with the active site and that the covalent bond is sufficiently stable for detection of the covalent rhomboid\u2010lactam complex. 4\u2010Oxo\u2010\u03b2\u2010lactams may therefore find future use as both inhibitors and activity\u2010based probes for rhomboid proteases.<\/jats:p>","DOI":"10.1002\/cbic.202300418","type":"journal-article","created":{"date-parts":[[2023,9,6]],"date-time":"2023-09-06T10:10:03Z","timestamp":1693995003000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["4\u2010Oxo\u2010\u03b2\u2010Lactams as Novel Inhibitors for Rhomboid Proteases"],"prefix":"10.1002","volume":"24","author":[{"given":"Jian","family":"Yang","sequence":"first","affiliation":[{"name":"Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine KU Leuven \u2013 University of Leuven  Herestraat 49, box 901b 3000 Leuven Belgium"}]},{"given":"Lu\u00eds A. 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