infections represent a great concern due to their versatility and involvement in different types of diseases. The shortage of available clinical options, especially to treat multiresistant strains, makes the discovery of new effective compounds essential. Here we describe the activity of the previously described cell division inhibitor C109 against methicillin-sensitive and -resistant strains. Antibiofilm activity was assessed using microtiter plates, confocal microscopy, and in an in vitro biofilm wound model. The ability of C109 to block FtsZ GTPase activity and polymerization was tested in vitro. Altogether, the results show that the FtsZ inhibitor C109 has activity against a wide range of strains and support its use as an antistaphylococcal compound.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8308607PMC
http://dx.doi.org/10.3390/pathogens10070886DOI Listing

Publication Analysis

Top Keywords

inhibitor c109
12
ftsz inhibitor
8
antistaphylococcal activity
4
activity ftsz
4
c109
4
c109 infections
4
infections represent
4
represent great
4
great concern
4
concern versatility
4

Similar Publications

More than half of the ~20,000 protein-encoding human genes have paralogs. Chemical proteomics has uncovered many electrophile-sensitive cysteines that are exclusive to subsets of paralogous proteins. Here we explore whether such covalent compound-cysteine interactions can be used to discover ligandable pockets in paralogs lacking the cysteine.

View Article and Find Full Text PDF

More than half of the ~20,000 protein-encoding human genes have at least one paralog. Chemical proteomics has uncovered many electrophile-sensitive cysteines that are exclusive to a subset of paralogous proteins. Here, we explore whether such covalent compound-cysteine interactions can be used to discover ligandable pockets in paralogs that lack the cysteine.

View Article and Find Full Text PDF

Bactericidal and Anti-Biofilm Activity of the FtsZ Inhibitor C109 against .

Antibiotics (Basel)

November 2022

Department of Biology and Biotechnology "Lazzaro Spallanzani", University of Pavia, 27100 Pavia, Italy.

In the last few years, has ranked as a number one priority due to its Multi Drug Resistant phenotype. The different metabolic states, such as the one adopted when growing as biofilm, help the bacterium to resist a wide variety of compounds, placing the discovery of new molecules able to counteract this pathogen as a topic of utmost importance. In this context, bacterial cell division machinery and the conserved protein FtsZ are considered very interesting cellular targets.

View Article and Find Full Text PDF

Antistaphylococcal Activity of the FtsZ Inhibitor C109.

Pathogens

July 2021

Department of Biology and Biotechnology "Lazzaro Spallanzani", University of Pavia, 27100 Pavia, Italy.

infections represent a great concern due to their versatility and involvement in different types of diseases. The shortage of available clinical options, especially to treat multiresistant strains, makes the discovery of new effective compounds essential. Here we describe the activity of the previously described cell division inhibitor C109 against methicillin-sensitive and -resistant strains.

View Article and Find Full Text PDF

Chemical, Metabolic, and Cellular Characterization of a FtsZ Inhibitor Effective Against .

Front Microbiol

April 2020

Laboratory of Molecular Microbiology, Department of Biology and Biotechnology "L. Spallanzani", University of Pavia, Pavia, Italy.

There is an urgent need for new antimicrobials to treat the opportunistic Gram-negative , which represents a problematic challenge for cystic fibrosis patients. Recently, a benzothiadiazole derivative, C109, was shown to be effective against the infections caused by and other Gram-negative and-positive bacteria. C109 has a promising cellular target, the cell division protein FtsZ, and a recently developed PEGylated formulation make it an attractive molecule to counteract infections.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!