Update on the discovery of efflux pump inhibitors against critical priority Gram-negative bacteria
N Compagne, A Vieira Da Cruz, RT Müller… - Antibiotics, 2023 - mdpi.com
Antimicrobial resistance (AMR) has become a major problem in public health leading to an
estimated 4.95 million deaths in 2019. The selective pressure caused by the massive and …
estimated 4.95 million deaths in 2019. The selective pressure caused by the massive and …
Mastering the Gram-negative bacterial barrier–Chemical approaches to increase bacterial bioavailability of antibiotics
HK Ropponen, R Richter, AKH Hirsch… - Advanced Drug Delivery …, 2021 - Elsevier
To win the battle against resistant, pathogenic bacteria, novel classes of anti-infectives and
targets are urgently needed. Bacterial uptake, distribution, metabolic and efflux pathways of …
targets are urgently needed. Bacterial uptake, distribution, metabolic and efflux pathways of …
A genetic platform to investigate the functions of bacterial drug efflux pumps
T Teelucksingh, LK Thompson, S Zhu… - Nature Chemical …, 2022 - nature.com
Efflux pumps are a serious challenge for the development of antibacterial agents.
Overcoming efflux requires an in-depth understanding of efflux pump functions, specificities …
Overcoming efflux requires an in-depth understanding of efflux pump functions, specificities …
The Gram-negative permeability barrier: tipping the balance of the in and the out
C Maher, KA Hassan - Mbio, 2023 - Am Soc Microbiol
Gram-negative bacteria are intrinsically resistant to many antibiotics, due in large part to the
permeability barrier formed by their cell envelope. The complex and synergistic interplay of …
permeability barrier formed by their cell envelope. The complex and synergistic interplay of …
Challenges in drug discovery for intracellular bacteria
Novel drugs are needed to treat a variety of persistent diseases caused by intracellular
bacterial pathogens. Virulence pathways enable many functions required for the survival of …
bacterial pathogens. Virulence pathways enable many functions required for the survival of …
Multidrug efflux in Gram-negative bacteria: structural modifications in active compounds leading to efflux pump avoidance
D Gurvic, U Zachariae - npj Antimicrobials and Resistance, 2024 - nature.com
Gram-negative bacteria cause the majority of critically drug-resistant infections,
necessitating the rapid development of new drugs with Gram-negative activity. However …
necessitating the rapid development of new drugs with Gram-negative activity. However …
Characterization of the hydrochloride salt hemihydrate as a new salt of the antifungal agent tioconazole
AB Moroni, EP Mayoral, DF Lionello, DR Vega… - International Journal of …, 2023 - Elsevier
Tioconazole is an effective antifungal agent, which has a very low solubility in aqueous
media, that limits its bioavailability and efficacy. In an effort to overcome the drug limitations …
media, that limits its bioavailability and efficacy. In an effort to overcome the drug limitations …
[HTML][HTML] A platform for predicting mechanism of action based on bacterial transcriptional responses identifies an unusual DNA gyrase inhibitor
In the search for much-needed new antibacterial chemical matter, a myriad of compounds
have been reported in academic and pharmaceutical screening endeavors. Only a small …
have been reported in academic and pharmaceutical screening endeavors. Only a small …
Proline-Hinged α-Helical Peptides Sensitize Gram-Positive Antibiotics, Expanding Their Physicochemical Properties to Be Used as Gram-Negative Antibiotics
Y Choi, HW Choe, M Kook, S Choo… - Journal of Medicinal …, 2023 - ACS Publications
The outer membrane (OM) of Gram-negative bacteria is the most difficult obstacle for small-
molecule antibiotics to reach their targets in the cytosol. The molecular features of Gram …
molecule antibiotics to reach their targets in the cytosol. The molecular features of Gram …
The inactivation of tolC sensitizes Escherichia coli to perturbations in lipopolysaccharide transport
S Zhu, MK Alexander, TO Paiva, K Rachwalski, A Miu… - Iscience, 2024 - cell.com
The Escherichia coli outer membrane channel TolC complexes with several inner
membrane efflux pumps to export compounds across the cell envelope. All components of …
membrane efflux pumps to export compounds across the cell envelope. All components of …