Ronald E. Painter
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View article: Antibacterial macrocyclic peptides reveal a distinct mode of BamA inhibition
Antibacterial macrocyclic peptides reveal a distinct mode of BamA inhibition Open
Outer membrane proteins (OMPs) produced by Gram-negative bacteria contain a cylindrical amphipathic β-sheet (“β-barrel”) that functions as a membrane spanning domain. The assembly (folding and membrane insertion) of OMPs is mediated by the…
View article: Structural characterization of a novel class of antibacterials that target the lipopolysaccharide transporter MsbA in multidrug-resistant <i>Acinetobacter baumannii</i>
Structural characterization of a novel class of antibacterials that target the lipopolysaccharide transporter MsbA in multidrug-resistant <i>Acinetobacter baumannii</i> Open
Acinetobacter baumannii is a Gram-negative pathogen responsible for pneumonia and wound, bloodstream, and urinary tract infections, particularly for patients in intensive care units. Using phenotypic screening we have identified a novel cl…
View article: Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration Open
The use of β-lactam (BL) and β-lactamase inhibitor combination to overcome BL antibiotic resistance has been validated through clinically approved drug products. However, unmet medical needs still exist for the treatment of infections caus…
View article: Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates Open
With the emergence and rapid spreading of NDM-1 and existence of clinically relevant VIM-1 and IMP-1, discovery of pan inhibitors targeting metallo-beta-lactamases (MBLs) became critical in our battle against bacterial infection. Concurren…
View article: Imipenem/Relebactam Resistance in Clinical Isolates of Extensively Drug Resistant Pseudomonas aeruginosa: Inhibitor-Resistant β-Lactamases and Their Increasing Importance
Imipenem/Relebactam Resistance in Clinical Isolates of Extensively Drug Resistant Pseudomonas aeruginosa: Inhibitor-Resistant β-Lactamases and Their Increasing Importance Open
Multidrug-resistant (MDR) Pseudomonas aeruginosa infections are a major clinical challenge. Many isolates are carbapenem resistant, which severely limits treatment options; thus, novel therapeutic combinations, such as imipenem-relebactam …
View article: A small-molecule inhibitor of BamA impervious to efflux and the outer membrane permeability barrier
A small-molecule inhibitor of BamA impervious to efflux and the outer membrane permeability barrier Open
Significance The spread of multidrug-resistant infections demands antibiotic development. Although new antibiotics targeting gram-positive bacteria have been developed, it has been more than 50 y since a new class of antibiotics targeting …
View article: Inhibitor of intramembrane protease RseP blocks the σ <sup>E</sup> response causing lethal accumulation of unfolded outer membrane proteins
Inhibitor of intramembrane protease RseP blocks the σ <sup>E</sup> response causing lethal accumulation of unfolded outer membrane proteins Open
Significance The σ E stress response monitors outer membrane protein (OMP) assembly. Uninduced, σ E is sequestered to the plasma membrane by its anti-sigma factor, RseA. Mutations perturbing OMP biogenesis induce degradation of RseA by the…
View article: Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase
Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase Open
To combat the threat of antibiotic-resistant Gram-negative bacteria, novel agents that circumvent established resistance mechanisms are urgently needed. Our approach was to focus first on identifying bioactive small molecules followed by c…
View article: Affinity Selection–Mass Spectrometry Identifies a Novel Antibacterial RNA Polymerase Inhibitor
Affinity Selection–Mass Spectrometry Identifies a Novel Antibacterial RNA Polymerase Inhibitor Open
The growing prevalence of drug resistant bacteria is a significant global threat to human health. The antibacterial drug rifampin, which functions by inhibiting bacterial RNA polymerase (RNAP), is an important part of the antibacterial arm…