Siderophore conjugation with cleavable linkers boosts the potency of RNA polymerase inhibitors against multidrug-resistant<i>E. coli</i>
Carsten Peukert, Anna C. Vetter, Hazel L. S. Fuchs, Kirsten Harmrolfs, Bianka Karge, Marc Stadler, Mark Brönstrup
Abstract
, 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.
Topics & Concepts
BiochemistryLinkerSiderophoreChemistryRNA polymeraseBacteriaAntibioticsBiologyRNAComputer scienceOperating systemGeneticsGeneAntibiotic Resistance in BacteriaBacterial Genetics and BiotechnologyBacteriophages and microbial interactions