Inhibitor of intramembrane protease RseP blocks the σ response causing lethal accumulation of unfolded outer membrane proteins. Author Anna Konovalova, Marcin Grabowicz, Carl Balibar, Juliana Malinverni, Ronald Painter, Daniel Riley, Paul Mann, Hao Wang, Charles Garlisi, Brad Sherborne, Nathan Rigel, Dante Ricci, Todd Black, Terry Roemer, Thomas Silhavy, Scott Walker Publication Year 2018 Type Journal Article Abstract The outer membrane (OM) of Gram-negative bacteria forms a robust permeability barrier that blocks entry of toxins and antibiotics. Most OM proteins (OMPs) assume a β-barrel fold, and some form aqueous channels for nutrient uptake and efflux of intracellular toxins. The Bam machine catalyzes rapid folding and assembly of OMPs. Fidelity of OMP biogenesis is monitored by the σ stress response. When OMP folding defects arise, the proteases DegS and RseP act sequentially to liberate σ into the cytosol, enabling it to activate transcription of the stress regulon. Here, we identify batimastat as a selective inhibitor of RseP that causes a lethal decrease in σ activity in , and we further identify RseP mutants that are insensitive to inhibition and confer resistance. Remarkably, batimastat treatment allows the capture of elusive intermediates in the OMP biogenesis pathway and offers opportunities to better understand the underlying basis for σ essentiality. Keywords Escherichia coli, Transcription Factors, Membrane Proteins, Escherichia coli Proteins, Bacterial Outer Membrane Proteins, Endopeptidases, Protein Unfolding Journal Proc Natl Acad Sci U S A Volume 115 Issue 28 Pages E6614-E6621 Date Published 2018 Jul 10 ISSN Number 1091-6490 DOI 10.1073/pnas.1806107115 Alternate Journal Proc Natl Acad Sci U S A PMCID PMC6048503 PMID 29941590 PubMedPubMed CentralGoogle ScholarBibTeXEndNote X3 XML