Selective toxicity of antibacterial agents—still a valid concept or do we miss chances and ignore risks?

A Dalhoff - Infection, 2021 - Springer
Background Selective toxicity antibacteribiotics is considered to be due to interactions with
targets either being unique to bacteria or being characterized by a dichotomy between pro …

Design of nanoparticle-based systems for the systemic delivery of chemotherapeutics: Alternative potential routes via sublingual and buccal administration for …

K Bahrami, E Lee, B Morse, OL Lanier… - Drug Delivery and …, 2024 - Springer
Conventional therapeutic approaches for cancer generally involve chemo-and radiation
therapies that often exhibit low efficacy and induce toxic side effects. Recent years have …

[HTML][HTML] Deterministic evolution and stringent selection during preneoplasia

K Karlsson, MJ Przybilla, E Kotler, A Khan, H Xu… - Nature, 2023 - nature.com
The earliest events during human tumour initiation, although poorly characterized, may hold
clues to malignancy detection and prevention. Here we model occult preneoplasia by …

Twist and turn—topoisomerase functions in mitochondrial DNA maintenance

S Goffart, A Hangas, JLO Pohjoismäki - International Journal of Molecular …, 2019 - mdpi.com
Like any genome, mitochondrial DNA (mtDNA) also requires the action of topoisomerases to
resolve topological problems in its maintenance, but for a long time, little was known about …

Zebrafish as an In Vivo High-Throughput Model for Genotoxicity

S Chakravarthy, S Sadagopan, A Nair, SK Sukumaran - Zebrafish, 2014 - liebertpub.com
Compounds routinely used to increase the quality of life and combat disease undergo
stringent potency and biosafety tests before approval. However, based on the outcome of …

DNA damage signaling assessed in individual cells in relation to the cell cycle phase and induction of apoptosis

Z Darzynkiewicz, H Zhao, HD Halicka… - Critical reviews in …, 2012 - Taylor & Francis
Reviewed are the phosphorylation events reporting activation of protein kinases and the key
substrates critical for the DNA damage signaling (DDS). These DDS events are detected …

Experimental evolution in TP53 deficient human gastric organoids recapitulates tumorigenesis

K Karlsson, M Przybilla, H Xu, E Kotler, K Karagyozova… - BioRxiv, 2022 - biorxiv.org
The earliest events during human tumor initiation, while poorly characterized, may hold
clues to malignancy detection and prevention. Here we model occult pre-neoplasia by bi …

[HTML][HTML] A high-throughput fluorescence anisotropy-based assay for human topoisomerase II β-catalyzed ATP-dependent supercoiled DNA relaxation

AB Shapiro, CA Austin - Analytical biochemistry, 2014 - Elsevier
Because of their essentiality for DNA replication, transcription, and repair, type II
topoisomerases are targets for antibacterial and anticancer drugs. There are two type II …

Cellular pharmacokinetics and intracellular activity of gepotidacin against Staphylococcus aureus isolates with different resistance phenotypes in models of cultured …

F Peyrusson, PM Tulkens… - Antimicrobial Agents and …, 2018 - Am Soc Microbiol
ABSTRACT Gepotidacin (GSK2140944), a novel triazaacenaphthylene bacterial
topoisomerase inhibitor, is currently in clinical development for the treatment of bacterial …

Pharmacodynamic profile of GSK2140944 against methicillin-resistant Staphylococcus aureus in a murine lung infection model

W So, JL Crandon, DP Nicolau - Antimicrobial Agents and …, 2015 - Am Soc Microbiol
ABSTRACT GSK2140944 is a novel bacterial type II topoisomerase inhibitor with in vitro
activity against key causative respiratory pathogens, including methicillin-resistant …