[HTML][HTML] Towards the sustainable discovery and development of new antibiotics

M Miethke, M Pieroni, T Weber, M Brönstrup… - Nature Reviews …, 2021 - nature.com
An ever-increasing demand for novel antimicrobials to treat life-threatening infections
caused by the global spread of multidrug-resistant bacterial pathogens stands in stark …

Fragment-to-lead medicinal chemistry publications in 2020

IJP De Esch, DA Erlanson, W Jahnke… - Journal of medicinal …, 2021 - ACS Publications
Fragment-based drug discovery (FBDD) continues to evolve and make an impact in the
pharmaceutical sciences. We summarize successful fragment-to-lead studies that were …

Moonlighting chaperone activity of the enzyme PqsE contributes to RhlR-controlled virulence of Pseudomonas aeruginosa

SR Borgert, S Henke, F Witzgall, S Schmelz… - Nature …, 2022 - nature.com
Pseudomonas aeruginosa is a major cause of nosocomial infections and also leads to
severe exacerbations in cystic fibrosis or chronic obstructive pulmonary disease. Three …

Quorum Sensing Inhibitors to Quench P. aeruginosa Pathogenicity

M Duplantier, E Lohou, P Sonnet - Pharmaceuticals, 2021 - mdpi.com
The emergence and the dissemination of multidrug-resistant bacteria constitute a major
public health issue. Among incriminated Gram-negative bacteria, Pseudomonas aeruginosa …

Fragment-to-lead medicinal chemistry publications in 2019

W Jahnke, DA Erlanson, IJP De Esch… - Journal of medicinal …, 2020 - ACS Publications
Fragment-based drug discovery (FBDD) has grown and matured to a point where it is
valuable to keep track of its extent and details of application. This Perspective summarizes …

Cilostazol is a promising anti-pseudomonal virulence drug by disruption of quorum sensing

MW Al-Rabia, HZ Asfour, NA Alhakamy, MA Bazuhair… - AMB Express, 2024 - Springer
Resistance to antibiotics is a critical growing public health problem that desires urgent action
to combat. To avoid the stress on bacterial growth that evokes the resistance development …

[HTML][HTML] Novel quinazolinone inhibitors of the Pseudomonas aeruginosa quorum sensing transcriptional regulator PqsR

S Grossman, F Soukarieh, W Richardson, R Liu… - European Journal of …, 2020 - Elsevier
Rising numbers of cases of multidrug-and extensively drug-resistant Pseudomonas
aeruginosa over recent years have created an urgent need for novel therapeutic …

Towards Translation of PqsR Inverse Agonists: From In Vitro Efficacy Optimization to In Vivo Proof‐of‐Principle

MM Hamed, AS Abdelsamie, K Rox, C Schütz… - Advanced …, 2023 - Wiley Online Library
Pseudomonas aeruginosa (PA) is an opportunistic human pathogen, which is involved in a
wide range of dangerous infections. It develops alarming resistances toward antibiotic …

Versatility and complexity: common and uncommon facets of LysR-type transcriptional regulators

AC Baugh, C Momany, EL Neidle - Annual Review of …, 2023 - annualreviews.org
LysR-type transcriptional regulators (LTTRs) form one of the largest families of bacterial
regulators. They are widely distributed and contribute to all aspects of metabolism and …

Drug Repurposing Targeting Pseudomonas aeruginosa MvfR Using Docking, Virtual Screening, Molecular Dynamics, and Free-Energy Calculations

TF Vieira, RP Magalhães, M Simões, SF Sousa - Antibiotics, 2022 - mdpi.com
Pseudomonas aeruginosa is an opportunistic Gram-negative bacterium responsible for
acute and chronic infections in planktonic state or in biofilms. The sessile structures are …