Chemical Science · 2023 · 19 citations · 34 references
Life SciencesMedicinal ChemistryPharmacologyAntimicrobial ResistanceDrug DesignDrug DiscoveryAntibacterial PharmacologyAntibiotic ResistanceAntibiotic Resistance MechanismsEnzyme InhibitionMultidrug ResistanceResistance In Gram-negative BacteriaAntibiotic DiscoveryCleavable LinkersConjugationMicrobial Iron UptakeMultidrug-resistant Gram-negative BacteriaMultidrug-resistant OrganismsNovel Antibacterial Drug DiscoveryTargeted Antibacterial Therapy
, and a combination of subcellular fractionation and quantitative mass spectrometry proved cellular uptake of the conjugate, release of the antibiotic, and its increased accumulation in the cytosol of bacteria. The study demonstrates how the potency of existing antibiotics against resistant Gram-negative pathogens can be boosted by adding functions for active transport and intracellular release.
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Predictive compound accumulation rules yield a broad-spectrum antibiotic
Michelle F. Richter, Bryon Drown, Andrew P. Riley et al. · Nature · 2017 · 886 citations
Novel antibody–antibiotic conjugate eliminates intracellular S. aureus
Sophie M. Lehar, Thomas H. Pillow, Min Xu et al. · Nature · 2015 · 833 citations
Simon Portsmouth, David van Veenhuyzen, Roger Echols et al. · The Lancet Infectious Diseases · 2018 · 404 citations