FtsZ, a bacterial cell-division protein, is an attractive antibacterial target. In the screening for an inhibitor of FtsZ, madurahydroxylactone () and its related derivatives 2-5 were isolated from sp. AN100570. Compound 1 inhibited FtsZ with an IC of 53.4 μM and showed potent antibacterial activity against and MRSA with an MIC of 1 μg/ml, whereas 2-5 were weak or inactive. Importantly, 1 induced cell elongation in the cell division phenotype assay, whereas 2-5 did not. It indicates that 1 exhibits its potent antibacterial activity via inhibition of FtsZ, and the hydroxyl group and hydroxylactone ring of 1 are critical for the activity. Thus, madurahydroxylactone is a new type of inhibitor of FtsZ.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.4014/jmb.1708.08044 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Magnolol as an Antibacterial Agent Against Drug-resistant Bacteria Targeting Filamentous Temperature-sensitive Mutant Z.
Chem Biodivers
December 2024
State Key Laboratory of Chemical Biology and Drug Discovery, and Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, P. R. China.
The emergence of multiple drug-resistant bacteria poses critical health threats worldwide. It is urgently needed to develop potent and safe antibacterial agents with novel bactericidal mechanisms to treat these infections. In this study, magnolol was identified as a potential bacterial cell division inhibitor by a cell-based screening approach.
View Article and Find Full Text PDFThe relation in MreB and intrabacterial nanotransportation system for VacA in Helicobacter pylori.
Med Mol Morphol
December 2024
Project Team for Study of Nanotransportation System, Center for Medical Research and Development, Osaka Medical and Pharmaceutical University, 2-7 Daigaku-Machi, Takatsuki, Osaka, 569-8686, Japan.
Helicobacter pylori possesses an intrabacterial nanotransportation system (ibNoTS) for transporting VacA, CagA, and urease within the bacterial cytoplasm. This system is controlled by the extrabacterial environment. The transport routes of the system for VacA have not yet been studied in detail.
View Article and Find Full Text PDFIsatin Bis-Imidathiazole Hybrids Identified as FtsZ Inhibitors with On-Target Activity Against .
Antibiotics (Basel)
October 2024
Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Article Synopsis
- * Certain compounds showed strong inhibitory effects (13.8-90.1 µM) without harming human epithelial or red blood cells, with the most effective derivative undergoing further testing for its anti-biofilm properties and impact on methicillin-resistant bacteria.
- * Analysis included a structure-activity relationship study to identify key structural features for antibacterial effectiveness, alongside molecular modeling that revealed how the active compound inhibits the FtsZ protein crucial for bacterial cell division.
Overexpression of l,d-Transpeptidase A Induces Dispensability of Rod Complex in .
ACS Infect Dis
November 2024
Department of Biosciences and Bioengineering, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand 247 667, India.
Antimicrobial resistance (AMR) is a significant global threat, and the presence of resistance-determinant genes is one of the major driving forces behind it. The bacterial rod complex is an essential set of proteins that is crucial for cell survival due to its role in cell wall biogenesis and shape maintenance. Therefore, these proteins offer excellent potential as drug targets; however, compensatory mutations in nontarget genes render this complex nonessential.
View Article and Find Full Text PDFRecent advances in studies on FtsZ inhibitors.
Biochem Pharmacol
December 2024
Department of Biochemical Pharmacy, School of Pharmacy, Second Military Medical University/Naval Medical University, Shanghai 200433, PR China. Electronic address:
Article Synopsis
- The emergence of multidrug-resistant bacteria due to antibiotic abuse has created an urgent demand for new antimicrobial drugs.
- FtsZ is a crucial protein in bacterial cell division and is becoming a promising target for the development of new antibiotics.
- The paper reviews various natural and synthetic compounds that can inhibit FtsZ, highlighting its potential role in the discovery of novel antibacterial drugs.
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!